LOXO ONCOLOGY

At Loxo Oncology, we are motivated by our goal of improving the lives of people living with cancer. Our team members choose to be part of Loxo Oncology because we share this passion and believe in our values. If our passion and values resonate with you, Loxo Oncology may be in your DNA. Learn more about current opportunities with Loxo Oncology. LIFE AT LOXO ONCOLOGY Josh Ballard Research Fellow, Biochemistry. "Loxo Oncology at Lilly leverages the capabilities and breadth of experience from Lilly while maintaining a nimble, patient-centered biotech mindset. The culture is anchored in significant collaboration and real-time, patient-centric decision making. For people who like working in an environment that LOXO-305, A NEXT GENERATION, HIGHLY SELECTIVE, NON LOXO-305 is a Highly Potent and Selective Non-Covalent BTK Inhibitor. Kinome selectivity. Highly selective for BTK. Xenograft models. In vivo . activity similarly efficacious as

MANAGEMENT TEAM

The Loxo Oncology management team is motivated by one goal: to dramatically improve the lives of people living with cancer. PRECLINICAL CHARACTERIZATION OF LOXO-338, A NOVEL, ORAL Preclinical characterization of LOXO-338, a novel, oral and selective BCL2 inhibitor Presented at: AACR Annual Meeting 2021 Date: April 10,

2021

CAREER OPPORTUNITIES Patients are at the heart of everything we do at Loxo Oncology, and we continue to be motivated by our goal of improving the lives of people

living with cancer.

PRE-CLINICAL CHARACTERIZATION OF POTENT AND SELECTIVE NEXT Crystal structure of selpercatinib (gray) bound to RET V804M (V804M gatekeeper residue shown in green). Selpercatinib is a potent inhibitor of RET V804M. RESULTS FROM THE FIRST-IN-HUMAN, PROOF-OF-CONCEPT PHASE 1 Presented at: 2019 ASH Annual Meeting Date: December 8, 2019. Results from the First-in-Human, Proof-of-Concept . Phase 1 BRUIN Trial in Pretreated B -Cell Malignancies for LOXO- 305, a Next- Generation, PRECLINICAL CHARACTERIZATION OF LY3484356, A NOVEL, POTENT 0 7 14 21 0 400 800 1200 1600. Treatment Days. Tumor Volume (mm. 3) ST941PBR ESR1 Y537S (palbociclib resistant) 47 54 61 68 0 200 400 600. Treatment Days. Tumor Volume (mm PRECLINICAL CHARACTERIZATION OF LY3537982, A NOVEL, HIGHLY Preclinical characterization of LY3537982, a novel, highly selective and potent KRAS-G12C inhibitor Presented at: AACR Annual Meeting 2021 Date: April 10, 2021

LOXO ONCOLOGY

At Loxo Oncology, we are motivated by our goal of improving the lives of people living with cancer. Our team members choose to be part of Loxo Oncology because we share this passion and believe in our values. If our passion and values resonate with you, Loxo Oncology may be in your DNA. Learn more about current opportunities with Loxo Oncology. LIFE AT LOXO ONCOLOGY Josh Ballard Research Fellow, Biochemistry. "Loxo Oncology at Lilly leverages the capabilities and breadth of experience from Lilly while maintaining a nimble, patient-centered biotech mindset. The culture is anchored in significant collaboration and real-time, patient-centric decision making. For people who like working in an environment that LOXO-305, A NEXT GENERATION, HIGHLY SELECTIVE, NON LOXO-305 is a Highly Potent and Selective Non-Covalent BTK Inhibitor. Kinome selectivity. Highly selective for BTK. Xenograft models. In vivo . activity similarly efficacious as

MANAGEMENT TEAM

The Loxo Oncology management team is motivated by one goal: to dramatically improve the lives of people living with cancer. PRECLINICAL CHARACTERIZATION OF LOXO-338, A NOVEL, ORAL Preclinical characterization of LOXO-338, a novel, oral and selective BCL2 inhibitor Presented at: AACR Annual Meeting 2021 Date: April 10,

2021

CAREER OPPORTUNITIES Patients are at the heart of everything we do at Loxo Oncology, and we continue to be motivated by our goal of improving the lives of people

living with cancer.

PRE-CLINICAL CHARACTERIZATION OF POTENT AND SELECTIVE NEXT Crystal structure of selpercatinib (gray) bound to RET V804M (V804M gatekeeper residue shown in green). Selpercatinib is a potent inhibitor of RET V804M. RESULTS FROM THE FIRST-IN-HUMAN, PROOF-OF-CONCEPT PHASE 1 Presented at: 2019 ASH Annual Meeting Date: December 8, 2019. Results from the First-in-Human, Proof-of-Concept . Phase 1 BRUIN Trial in Pretreated B -Cell Malignancies for LOXO- 305, a Next- Generation, PRECLINICAL CHARACTERIZATION OF LY3484356, A NOVEL, POTENT 0 7 14 21 0 400 800 1200 1600. Treatment Days. Tumor Volume (mm. 3) ST941PBR ESR1 Y537S (palbociclib resistant) 47 54 61 68 0 200 400 600. Treatment Days. Tumor Volume (mm PRECLINICAL CHARACTERIZATION OF LY3537982, A NOVEL, HIGHLY Preclinical characterization of LY3537982, a novel, highly selective and potent KRAS-G12C inhibitor Presented at: AACR Annual Meeting 2021 Date: April 10, 2021 CAREER OPPORTUNITIES Loxo Oncology, Inc. (Loxo) currently anticipates that the base salary for the Associate Scientist level could range from between $59,000 to $86,577 and that the base salary for the Scientist level could range from between $78,000 to $114,498 will depend, in part, on the successful candidate’s qualifications for the role, including education and experience. PIPELINE | LOXO ONCOLOGY Pipeline Overview. Loxo Oncology at Lilly seeks to discover and develop a broad pipeline of treatments with the potential to make a meaningful difference for people living with cancer. The safety and efficacy of the agents and uses under investigation have not been

established.

LOXO-305 (BTK INHIBITOR) Pirtobrutinib (LOXO-305) Pirtobrutinib is an investigational, oral, highly-selective non-covalent Bruton’s tyrosine kinase (BTK) inhibitor. BTK plays a key role in the B-cell antigen receptor signaling pathway, which is required for the development, activation and survival of normal white blood cells, known as B-cells, and

malignant B-cells.

PUBLICATIONS & PRESENTATIONS Publications from Loxo Oncology. LOXO-305, a Next Generation, Highly Selective, NonCovalent BTK Inhibitor in Previously Treated Mantle Cell Lymphoma, Waldenstrom's Macroglobulinemia, and Other Non-Hodgkin Lymphomas: Results from the Phase 1/2 BRUIN Study IN VIVO PRE-CLINICAL EVALUATION OF LOXO- 305 ALONE AND IN Presented at: 2020 ASH Annual Meeting Date: December 7, 2020. In Vivo Pre-Clinical Evaluation of LOXO- 305 Alone and in Combination with Venetoclax, R-CHOP or RESULTS FROM THE FIRST-IN-HUMAN, PROOF-OF-CONCEPT PHASE 1 Presented at: 2019 ASH Annual Meeting Date: December 8, 2019. Results from the First-in-Human, Proof-of-Concept . Phase 1 BRUIN Trial in Pretreated B -Cell Malignancies for LOXO- 305, a Next- Generation, A FIRST-IN-HUMAN PHASE 1A/B TRIAL OF LY3484356, AN ORAL Presented at: ASCO Annual Meeting 2021 Date: June 4, 2021. A first-in-human phase 1a/b trial of LY3484356, an oral selective estrogen receptor (ER) degrader (SERD) in CLINICAL SAFETY AND ACTIVITY FROM A PHASE 1 STUDY OF LOXO Clinical safety and activity from a Phase 1 study of LOXO-101, a selective TRKA/B/C inhibitor, in solid-tumor patients with NTRK gene fusions David S. Hong1, Anna F. Farago2,Marcia S. Brose3, Howard A. Burris, III4, Afshin Dowlati5, Todd M. Bauer4, Matthew Taylor6, Alice T. Shaw2,Adriana Estrada-Bernal7, Anh T. Le7, Nisha Nanda8, Michael C. Cox8, Robert C. Doebele7 THE EFFICACY OF LAROTRECTINIB (LOXO-101), A SELECTIVE The efficacy of larotrectinib (LOXO-101), a selective tropomyosin receptor kinase (TRK) inhibitor, in adult and pediatric TRK fusion cancers Hyman DM,1 Laetsch TW,2 Kummar S,3 DuBois SG,4 Farago AF,5 Pappo AS,6 Demetri GD,7 El-Deiry WS,8 Lassen UN,9 Dowlati A,10 Brose MS,11 Boni V,12 Turpin B,13 Nagasubramanian R,14 Cruickshank S,15 Cox MC, 15Ku NC, Hawkins DS,16 Hong DS,17 Drilon AE1 E I C PHARMACOKINETICS (PK) OF LOXO-101 DURING THE FIRST Introduction Baseline Characteristics Pharmacokinetics (PK) of LOXO-101 During the First-in-Human Phase I Study in Patients with Advanced Solid Tumors - Interim Update

LOXO ONCOLOGY

At Loxo Oncology, we are motivated by our goal of improving the lives of people living with cancer. Our team members choose to be part of Loxo Oncology because we share this passion and believe in our values. If our passion and values resonate with you, Loxo Oncology may be in your DNA. Learn more about current opportunities with Loxo Oncology. LOXO-305 (BTK INHIBITOR) Pirtobrutinib (LOXO-305) Pirtobrutinib is an investigational, oral, highly-selective non-covalent Bruton’s tyrosine kinase (BTK) inhibitor. BTK plays a key role in the B-cell antigen receptor signaling pathway, which is required for the development, activation and survival of normal white blood cells, known as B-cells, and

malignant B-cells.

CAREER OPPORTUNITIES Patients are at the heart of everything we do at Loxo Oncology, and we continue to be motivated by our goal of improving the lives of people

living with cancer.

PRECLINICAL CHARACTERIZATION OF LOXO-338, A NOVEL, ORAL Preclinical characterization of LOXO-338, a novel, oral and selective BCL2 inhibitor Presented at: AACR Annual Meeting 2021 Date: April 10,

2021

PRE-CLINICAL CHARACTERIZATION OF POTENT AND SELECTIVE NEXT Crystal structure of selpercatinib (gray) bound to RET V804M (V804M gatekeeper residue shown in green). Selpercatinib is a potent inhibitor of RET V804M. PRECLINICAL CHARACTERIZATION OF LY3484356, A NOVEL, POTENT 0 7 14 21 0 400 800 1200 1600. Treatment Days. Tumor Volume (mm. 3) ST941PBR ESR1 Y537S (palbociclib resistant) 47 54 61 68 0 200 400 600. Treatment Days. Tumor Volume (mm RESULTS FROM THE FIRST-IN-HUMAN, PROOF-OF-CONCEPT PHASE 1 Presented at: 2019 ASH Annual Meeting Date: December 8, 2019. Results from the First-in-Human, Proof-of-Concept . Phase 1 BRUIN Trial in Pretreated B -Cell Malignancies for LOXO- 305, a Next- Generation, PRECLINICAL CHARACTERIZATION OF LY3537982, A NOVEL, HIGHLY Preclinical characterization of LY3537982, a novel, highly selective and potent KRAS-G12C inhibitor Presented at: AACR Annual Meeting 2021 Date: April 10, 2021 CLINICAL SAFETY AND ACTIVITY FROM A PHASE 1 STUDY OF LOXO Clinical safety and activity from a Phase 1 study of LOXO-101, a selective TRKA/B/C inhibitor, in solid-tumor patients with NTRK gene fusions David S. Hong1, Anna F. Farago2,Marcia S. Brose3, Howard A. Burris, III4, Afshin Dowlati5, Todd M. Bauer4, Matthew Taylor6, Alice T. Shaw2,Adriana Estrada-Bernal7, Anh T. Le7, Nisha Nanda8, Michael C. Cox8, Robert C. Doebele7 D A Y - LOXO ONCOLOGY 0 5 1 0 1 5 0 2 0 0 4 0 0 6 0 0 8 0 0 1 0 0 0 N I H 3 T 3 K I F 5 B - R E T D a y T u m o r V o l u m e (m e a n S E M, m m 3) 0 5 1 0 1 5 0 5 0 0 1 0 0 0 1 5 0 0 2 0

LOXO ONCOLOGY

At Loxo Oncology, we are motivated by our goal of improving the lives of people living with cancer. Our team members choose to be part of Loxo Oncology because we share this passion and believe in our values. If our passion and values resonate with you, Loxo Oncology may be in your DNA. Learn more about current opportunities with Loxo Oncology. LOXO-305 (BTK INHIBITOR) Pirtobrutinib (LOXO-305) Pirtobrutinib is an investigational, oral, highly-selective non-covalent Bruton’s tyrosine kinase (BTK) inhibitor. BTK plays a key role in the B-cell antigen receptor signaling pathway, which is required for the development, activation and survival of normal white blood cells, known as B-cells, and

malignant B-cells.

CAREER OPPORTUNITIES Patients are at the heart of everything we do at Loxo Oncology, and we continue to be motivated by our goal of improving the lives of people

living with cancer.

PRECLINICAL CHARACTERIZATION OF LOXO-338, A NOVEL, ORAL Preclinical characterization of LOXO-338, a novel, oral and selective BCL2 inhibitor Presented at: AACR Annual Meeting 2021 Date: April 10,

2021

PRE-CLINICAL CHARACTERIZATION OF POTENT AND SELECTIVE NEXT Crystal structure of selpercatinib (gray) bound to RET V804M (V804M gatekeeper residue shown in green). Selpercatinib is a potent inhibitor of RET V804M. PRECLINICAL CHARACTERIZATION OF LY3484356, A NOVEL, POTENT 0 7 14 21 0 400 800 1200 1600. Treatment Days. Tumor Volume (mm. 3) ST941PBR ESR1 Y537S (palbociclib resistant) 47 54 61 68 0 200 400 600. Treatment Days. Tumor Volume (mm RESULTS FROM THE FIRST-IN-HUMAN, PROOF-OF-CONCEPT PHASE 1 Presented at: 2019 ASH Annual Meeting Date: December 8, 2019. Results from the First-in-Human, Proof-of-Concept . Phase 1 BRUIN Trial in Pretreated B -Cell Malignancies for LOXO- 305, a Next- Generation, PRECLINICAL CHARACTERIZATION OF LY3537982, A NOVEL, HIGHLY Preclinical characterization of LY3537982, a novel, highly selective and potent KRAS-G12C inhibitor Presented at: AACR Annual Meeting 2021 Date: April 10, 2021 CLINICAL SAFETY AND ACTIVITY FROM A PHASE 1 STUDY OF LOXO Clinical safety and activity from a Phase 1 study of LOXO-101, a selective TRKA/B/C inhibitor, in solid-tumor patients with NTRK gene fusions David S. Hong1, Anna F. Farago2,Marcia S. Brose3, Howard A. Burris, III4, Afshin Dowlati5, Todd M. Bauer4, Matthew Taylor6, Alice T. Shaw2,Adriana Estrada-Bernal7, Anh T. Le7, Nisha Nanda8, Michael C. Cox8, Robert C. Doebele7 D A Y - LOXO ONCOLOGY 0 5 1 0 1 5 0 2 0 0 4 0 0 6 0 0 8 0 0 1 0 0 0 N I H 3 T 3 K I F 5 B - R E T D a y T u m o r V o l u m e (m e a n S E M, m m 3) 0 5 1 0 1 5 0 5 0 0 1 0 0 0 1 5 0 0 2 0 LIFE AT LOXO ONCOLOGY Josh Ballard Research Fellow, Biochemistry. "Loxo Oncology at Lilly leverages the capabilities and breadth of experience from Lilly while maintaining a nimble, patient-centered biotech mindset. The culture is anchored in significant collaboration and real-time, patient-centric decision making. For people who like working in an environment that PARTNERS | LOXO ONCOLOGY Loxo Oncology at Lilly supports third-party research that is aimed at furthering scientific knowledge and understanding in oncology. Loxo Oncology at Lilly will assess proposals for providing study drug and/or financial support for Investigator-Initiated Research based on scientific merit and strategic fit with our areas of research

interest.

LY3484356 | LOXO ONCOLOGY LY3484356 is an investigational, oral selective estrogen receptor degrader (SERD) with pure antagonistic properties. The estrogen receptor (ER) is the key therapeutic target for patients with ER+/HER2- breast cancer. Novel degraders of ER may overcome endocrine therapy resistance while providing consistent oral pharmacology and

convenience of

CLINICAL SAFETY AND ACTIVITY FROM A PHASE 1 STUDY OF LOXO Clinical safety and activity from a Phase 1 study of LOXO-101, a selective TRKA/B/C inhibitor, in solid-tumor patients with NTRK gene fusions David S. Hong1, Anna F. Farago2,Marcia S. Brose3, Howard A. Burris, III4, Afshin Dowlati5, Todd M. Bauer4, Matthew Taylor6, Alice T. Shaw2,Adriana Estrada-Bernal7, Anh T. Le7, Nisha Nanda8, Michael C. Cox8, Robert C. Doebele7 FIRST EXPERIENCE OF LOXO-292 IN THE MANAGEMENT OF First experience of LOXO-292 in the management of pediatric patients with RET-altered cancers Gerdemann U,1 Lee YA,2 Henry D, 3Smith S,4 Ortiz MV,5 Rothenberg SM, Raju SG, Cox MC,4 Bender JLG,5 Pappo AS,6 Frazier AL,1 Kang HJ2 1Dana-Farber Cancer Institute, Boston, MA; 2Seoul National University College of Medicine, Seoul, Republic of Korea; 3Loxo Oncology, Inc, Stamford, CT; E I C PHARMACOKINETICS (PK) OF LOXO-101 DURING THE FIRST Introduction Baseline Characteristics Pharmacokinetics (PK) of LOXO-101 During the First-in-Human Phase I Study in Patients with Advanced Solid Tumors - Interim Update D A Y - LOXO ONCOLOGY 0 5 1 0 1 5 0 2 0 0 4 0 0 6 0 0 8 0 0 1 0 0 0 N I H 3 T 3 K I F 5 B - R E T D a y T u m o r V o l u m e (m e a n S E M, m m 3) 0 5 1 0 1 5 0 5 0 0 1 0 0 0 1 5 0 0 2 0 A PEDIATRIC PHASE 1 STUDY OF LAROTRECTINIB, A HIGHLY 4. Larotrectinib is the first and only selective pan-TRK inhibitor in clinical development • Larotrectinib is a highly potent and

selective small-

A PEDIATRIC PHASE 1 STUDY OF LAROTRECTINIB, A HIGHLY Pharmacokinetics 9 Concentration-time AUC 0–24 in patients treated with 80–125 mg/m2 BID Laetsch, 10510 0 1 10 100 tinib g/mL) 1000 3 6 Time (hours) 9 12 Adults (100 mg LAROTRECTINIB EFFICACY AND SAFETY IN TRK FUSION CANCER: AN • Larotrectinib is a highly potent small-molecule inhibitor of TRKA, TRKB, and TRKC (5–11 nM IC 50 in cellular assays) • Demonstrated activity in CNS disease

LOXO ONCOLOGY

At Loxo Oncology, we are motivated by our goal of improving the lives of people living with cancer. Our team members choose to be part of Loxo Oncology because we share this passion and believe in our values. If our passion and values resonate with you, Loxo Oncology may be in your DNA. Learn more about current opportunities with Loxo Oncology. LIFE AT LOXO ONCOLOGY Josh Ballard Research Fellow, Biochemistry. "Loxo Oncology at Lilly leverages the capabilities and breadth of experience from Lilly while maintaining a nimble, patient-centered biotech mindset. The culture is anchored in significant collaboration and real-time, patient-centric decision making. For people who like working in an environment that CAREER OPPORTUNITIES Loxo Oncology, Inc. (Loxo) currently anticipates that the base salary for this position could range from between $135,300 to $198,516 and will depend, in part, on the successful candidate’s qualifications for the role, including education and experience. LOXO-305 (BTK INHIBITOR) Pirtobrutinib (LOXO-305) Pirtobrutinib is an investigational, oral, highly-selective non-covalent Bruton’s tyrosine kinase (BTK) inhibitor. BTK plays a key role in the B-cell antigen receptor signaling pathway, which is required for the development, activation and survival of normal white blood cells, known as B-cells, and

malignant B-cells.

MANAGEMENT TEAM

The Loxo Oncology management team is motivated by one goal: to dramatically improve the lives of people living with cancer. CAREER OPPORTUNITIES Patients are at the heart of everything we do at Loxo Oncology, and we continue to be motivated by our goal of improving the lives of people

living with cancer.

PRECLINICAL CHARACTERIZATION OF LOXO-338, A NOVEL, ORAL Preclinical characterization of LOXO-338, a novel, oral and selective BCL2 inhibitor Presented at: AACR Annual Meeting 2021 Date: April 10,

2021

PRE-CLINICAL CHARACTERIZATION OF POTENT AND SELECTIVE NEXT Crystal structure of selpercatinib (gray) bound to RET V804M (V804M gatekeeper residue shown in green). Selpercatinib is a potent inhibitor of RET V804M. RESULTS FROM THE FIRST-IN-HUMAN, PROOF-OF-CONCEPT PHASE 1 Presented at: 2019 ASH Annual Meeting Date: December 8, 2019. Results from the First-in-Human, Proof-of-Concept . Phase 1 BRUIN Trial in Pretreated B -Cell Malignancies for LOXO- 305, a Next- Generation, A PEDIATRIC PHASE 1 STUDY OF LAROTRECTINIB, A HIGHLY Pharmacokinetics 9 Concentration-time AUC 0–24 in patients treated with 80–125 mg/m2 BID Laetsch, 10510 0 1 10 100 tinib g/mL) 1000 3 6 Time (hours) 9 12 Adults (100 mg

LOXO ONCOLOGY

At Loxo Oncology, we are motivated by our goal of improving the lives of people living with cancer. Our team members choose to be part of Loxo Oncology because we share this passion and believe in our values. If our passion and values resonate with you, Loxo Oncology may be in your DNA. Learn more about current opportunities with Loxo Oncology. LIFE AT LOXO ONCOLOGY Josh Ballard Research Fellow, Biochemistry. "Loxo Oncology at Lilly leverages the capabilities and breadth of experience from Lilly while maintaining a nimble, patient-centered biotech mindset. The culture is anchored in significant collaboration and real-time, patient-centric decision making. For people who like working in an environment that CAREER OPPORTUNITIES Loxo Oncology, Inc. (Loxo) currently anticipates that the base salary for this position could range from between $135,300 to $198,516 and will depend, in part, on the successful candidate’s qualifications for the role, including education and experience. LOXO-305 (BTK INHIBITOR) Pirtobrutinib (LOXO-305) Pirtobrutinib is an investigational, oral, highly-selective non-covalent Bruton’s tyrosine kinase (BTK) inhibitor. BTK plays a key role in the B-cell antigen receptor signaling pathway, which is required for the development, activation and survival of normal white blood cells, known as B-cells, and

malignant B-cells.

MANAGEMENT TEAM

The Loxo Oncology management team is motivated by one goal: to dramatically improve the lives of people living with cancer. CAREER OPPORTUNITIES Patients are at the heart of everything we do at Loxo Oncology, and we continue to be motivated by our goal of improving the lives of people

living with cancer.

PRECLINICAL CHARACTERIZATION OF LOXO-338, A NOVEL, ORAL Preclinical characterization of LOXO-338, a novel, oral and selective BCL2 inhibitor Presented at: AACR Annual Meeting 2021 Date: April 10,

2021

PRE-CLINICAL CHARACTERIZATION OF POTENT AND SELECTIVE NEXT Crystal structure of selpercatinib (gray) bound to RET V804M (V804M gatekeeper residue shown in green). Selpercatinib is a potent inhibitor of RET V804M. RESULTS FROM THE FIRST-IN-HUMAN, PROOF-OF-CONCEPT PHASE 1 Presented at: 2019 ASH Annual Meeting Date: December 8, 2019. Results from the First-in-Human, Proof-of-Concept . Phase 1 BRUIN Trial in Pretreated B -Cell Malignancies for LOXO- 305, a Next- Generation, A PEDIATRIC PHASE 1 STUDY OF LAROTRECTINIB, A HIGHLY Pharmacokinetics 9 Concentration-time AUC 0–24 in patients treated with 80–125 mg/m2 BID Laetsch, 10510 0 1 10 100 tinib g/mL) 1000 3 6 Time (hours) 9 12 Adults (100 mg PARTNERS | LOXO ONCOLOGY Loxo Oncology at Lilly supports third-party research that is aimed at furthering scientific knowledge and understanding in oncology. Loxo Oncology at Lilly will assess proposals for providing study drug and/or financial support for Investigator-Initiated Research based on scientific merit and strategic fit with our areas of research

interest.

PIPELINE | LOXO ONCOLOGY Pipeline Overview. Loxo Oncology at Lilly seeks to discover and develop a broad pipeline of treatments with the potential to make a meaningful difference for people living with cancer. The safety and efficacy of the agents and uses under investigation have not been

established.

PIPELINE | LOXO ONCOLOGY Pipeline Overview. Loxo Oncology at Lilly seeks to discover and develop a broad pipeline of treatments with the potential to make a meaningful difference for people living with cancer. LY3484356 | LOXO ONCOLOGY LY3484356 is an investigational, oral selective estrogen receptor degrader (SERD) with pure antagonistic properties. The estrogen receptor (ER) is the key therapeutic target for patients with

ER+/HER2-

PRE-CLINICAL CHARACTERIZATION OF POTENT AND SELECTIVE NEXT Crystal structure of selpercatinib (gray) bound to RET V804M (V804M gatekeeper residue shown in green). Selpercatinib is a potent inhibitor of RET V804M. A FIRST-IN-HUMAN PHASE 1A/B TRIAL OF LY3484356, AN ORAL Presented at: ASCO Annual Meeting 2021 Date: June 4, 2021. A first-in-human phase 1a/b trial of LY3484356, an oral selective estrogen receptor (ER) degrader (SERD) in RESULTS FROM THE FIRST-IN-HUMAN, PROOF-OF-CONCEPT PHASE 1 Presented at: 2019 ASH Annual Meeting Date: December 8, 2019. Results from the First-in-Human, Proof-of-Concept . Phase 1 BRUIN Trial in Pretreated B -Cell Malignancies for LOXO- 305, a Next- Generation, CLINICAL ACTIVITY OF LOXO-292, A HIGHLY SELECTIVE RET Clinical Activity of LOXO-292, a Highly Selective RET Inhibitor, in Patients with RET Fusion+ Non-Small Cell Lung Cancer An Update from ASCO 2018 Geoffrey R. Oxnard, Vivek Subbiah, Keunchil Park, Todd M. Bauer, Lori J. Wirth, Vamsidhar

TERMS OF USE

Such statements may be indicated by the use of words such as “anticipate,” “estimate,” “expect,” “project,” “intend,” “plan,” “believe,” and other terms of similar meaning appearing in discussions of future operating or financial performance. Such statements are based on company management’s current expectations CLINICAL SAFETY AND ACTIVITY FROM A PHASE 1 STUDY OF LOXO Clinical safety and activity from a Phase 1 study of LOXO-101, a selective TRKA/B/C inhibitor, in solid-tumor patients with NTRK gene fusions David S. Hong1, Anna F. Farago2,Marcia S. Brose3, Howard A. Burris, III4, Afshin Dowlati5, Todd M. Bauer4, Matthew Taylor6, Alice T. Shaw2,Adriana Estrada-Bernal7, Anh T. Le7, Nisha Nanda8, Michael C. Cox8, Robert C. Doebele7

LOXO ONCOLOGY

At Loxo Oncology, we are motivated by our goal of improving the lives of people living with cancer. Our team members choose to be part of Loxo Oncology because we share this passion and believe in our values. If our passion and values resonate with you, Loxo Oncology may be in your DNA. Learn more about current opportunities with Loxo Oncology. LIFE AT LOXO ONCOLOGY Josh Ballard Research Fellow, Biochemistry. "Loxo Oncology at Lilly leverages the capabilities and breadth of experience from Lilly while maintaining a nimble, patient-centered biotech mindset. The culture is anchored in significant collaboration and real-time, patient-centric decision making. For people who like working in an environment that CAREER OPPORTUNITIES Loxo Oncology, Inc. (Loxo) currently anticipates that the base salary for this position could range from between $135,300 to $198,516 and will depend, in part, on the successful candidate’s qualifications for the role, including education and experience. LOXO-305 (BTK INHIBITOR) Pirtobrutinib (LOXO-305) Pirtobrutinib is an investigational, oral, highly-selective non-covalent Bruton’s tyrosine kinase (BTK) inhibitor. BTK plays a key role in the B-cell antigen receptor signaling pathway, which is required for the development, activation and survival of normal white blood cells, known as B-cells, and

malignant B-cells.

MANAGEMENT TEAM

The Loxo Oncology management team is motivated by one goal: to dramatically improve the lives of people living with cancer. CAREER OPPORTUNITIES Patients are at the heart of everything we do at Loxo Oncology, and we continue to be motivated by our goal of improving the lives of people

living with cancer.

PRECLINICAL CHARACTERIZATION OF LOXO-338, A NOVEL, ORAL Preclinical characterization of LOXO-338, a novel, oral and selective BCL2 inhibitor Presented at: AACR Annual Meeting 2021 Date: April 10,

2021

PRE-CLINICAL CHARACTERIZATION OF POTENT AND SELECTIVE NEXT Crystal structure of selpercatinib (gray) bound to RET V804M (V804M gatekeeper residue shown in green). Selpercatinib is a potent inhibitor of RET V804M. RESULTS FROM THE FIRST-IN-HUMAN, PROOF-OF-CONCEPT PHASE 1LOXO 305 PDFLOXO 305 TRIALLATE BREAKING ABSTRACT LOXO 305LOXO 305 CLINICAL TRIALSLOXO 305 SIDE EFFECTSLOXO 305 STRUCTURE Presented at: 2019 ASH Annual Meeting Date: December 8, 2019. Results from the First-in-Human, Proof-of-Concept . Phase 1 BRUIN Trial in Pretreated B -Cell Malignancies for LOXO- 305, a Next- Generation, A PEDIATRIC PHASE 1 STUDY OF LAROTRECTINIB, A HIGHLY Pharmacokinetics 9 Concentration-time AUC 0–24 in patients treated with 80–125 mg/m2 BID Laetsch, 10510 0 1 10 100 tinib g/mL) 1000 3 6 Time (hours) 9 12 Adults (100 mg

LOXO ONCOLOGY

At Loxo Oncology, we are motivated by our goal of improving the lives of people living with cancer. Our team members choose to be part of Loxo Oncology because we share this passion and believe in our values. If our passion and values resonate with you, Loxo Oncology may be in your DNA. Learn more about current opportunities with Loxo Oncology. LIFE AT LOXO ONCOLOGY Josh Ballard Research Fellow, Biochemistry. "Loxo Oncology at Lilly leverages the capabilities and breadth of experience from Lilly while maintaining a nimble, patient-centered biotech mindset. The culture is anchored in significant collaboration and real-time, patient-centric decision making. For people who like working in an environment that CAREER OPPORTUNITIES Loxo Oncology, Inc. (Loxo) currently anticipates that the base salary for this position could range from between $135,300 to $198,516 and will depend, in part, on the successful candidate’s qualifications for the role, including education and experience. LOXO-305 (BTK INHIBITOR) Pirtobrutinib (LOXO-305) Pirtobrutinib is an investigational, oral, highly-selective non-covalent Bruton’s tyrosine kinase (BTK) inhibitor. BTK plays a key role in the B-cell antigen receptor signaling pathway, which is required for the development, activation and survival of normal white blood cells, known as B-cells, and

malignant B-cells.

MANAGEMENT TEAM

The Loxo Oncology management team is motivated by one goal: to dramatically improve the lives of people living with cancer. CAREER OPPORTUNITIES Patients are at the heart of everything we do at Loxo Oncology, and we continue to be motivated by our goal of improving the lives of people

living with cancer.

PRECLINICAL CHARACTERIZATION OF LOXO-338, A NOVEL, ORAL Preclinical characterization of LOXO-338, a novel, oral and selective BCL2 inhibitor Presented at: AACR Annual Meeting 2021 Date: April 10,

2021

PRE-CLINICAL CHARACTERIZATION OF POTENT AND SELECTIVE NEXT Crystal structure of selpercatinib (gray) bound to RET V804M (V804M gatekeeper residue shown in green). Selpercatinib is a potent inhibitor of RET V804M. RESULTS FROM THE FIRST-IN-HUMAN, PROOF-OF-CONCEPT PHASE 1LOXO 305 PDFLOXO 305 TRIALLATE BREAKING ABSTRACT LOXO 305LOXO 305 CLINICAL TRIALSLOXO 305 SIDE EFFECTSLOXO 305 STRUCTURE Presented at: 2019 ASH Annual Meeting Date: December 8, 2019. Results from the First-in-Human, Proof-of-Concept . Phase 1 BRUIN Trial in Pretreated B -Cell Malignancies for LOXO- 305, a Next- Generation, A PEDIATRIC PHASE 1 STUDY OF LAROTRECTINIB, A HIGHLY Pharmacokinetics 9 Concentration-time AUC 0–24 in patients treated with 80–125 mg/m2 BID Laetsch, 10510 0 1 10 100 tinib g/mL) 1000 3 6 Time (hours) 9 12 Adults (100 mg PARTNERS | LOXO ONCOLOGY Loxo Oncology at Lilly supports third-party research that is aimed at furthering scientific knowledge and understanding in oncology. Loxo Oncology at Lilly will assess proposals for providing study drug and/or financial support for Investigator-Initiated Research based on scientific merit and strategic fit with our areas of research

interest.

PIPELINE | LOXO ONCOLOGY Pipeline Overview. Loxo Oncology at Lilly seeks to discover and develop a broad pipeline of treatments with the potential to make a meaningful difference for people living with cancer. The safety and efficacy of the agents and uses under investigation have not been

established.

PIPELINE | LOXO ONCOLOGY Pipeline Overview. Loxo Oncology at Lilly seeks to discover and develop a broad pipeline of treatments with the potential to make a meaningful difference for people living with cancer. LY3484356 | LOXO ONCOLOGY LY3484356 is an investigational, oral selective estrogen receptor degrader (SERD) with pure antagonistic properties. The estrogen receptor (ER) is the key therapeutic target for patients with

ER+/HER2-

PRE-CLINICAL CHARACTERIZATION OF POTENT AND SELECTIVE NEXT Crystal structure of selpercatinib (gray) bound to RET V804M (V804M gatekeeper residue shown in green). Selpercatinib is a potent inhibitor of RET V804M. A FIRST-IN-HUMAN PHASE 1A/B TRIAL OF LY3484356, AN ORAL Presented at: ASCO Annual Meeting 2021 Date: June 4, 2021. A first-in-human phase 1a/b trial of LY3484356, an oral selective estrogen receptor (ER) degrader (SERD) in RESULTS FROM THE FIRST-IN-HUMAN, PROOF-OF-CONCEPT PHASE 1 Presented at: 2019 ASH Annual Meeting Date: December 8, 2019. Results from the First-in-Human, Proof-of-Concept . Phase 1 BRUIN Trial in Pretreated B -Cell Malignancies for LOXO- 305, a Next- Generation, CLINICAL ACTIVITY OF LOXO-292, A HIGHLY SELECTIVE RET Clinical Activity of LOXO-292, a Highly Selective RET Inhibitor, in Patients with RET Fusion+ Non-Small Cell Lung Cancer An Update from ASCO 2018 Geoffrey R. Oxnard, Vivek Subbiah, Keunchil Park, Todd M. Bauer, Lori J. Wirth, Vamsidhar

TERMS OF USE

Such statements may be indicated by the use of words such as “anticipate,” “estimate,” “expect,” “project,” “intend,” “plan,” “believe,” and other terms of similar meaning appearing in discussions of future operating or financial performance. Such statements are based on company management’s current expectations CLINICAL SAFETY AND ACTIVITY FROM A PHASE 1 STUDY OF LOXO Clinical safety and activity from a Phase 1 study of LOXO-101, a selective TRKA/B/C inhibitor, in solid-tumor patients with NTRK gene fusions David S. Hong1, Anna F. Farago2,Marcia S. Brose3, Howard A. Burris, III4, Afshin Dowlati5, Todd M. Bauer4, Matthew Taylor6, Alice T. Shaw2,Adriana Estrada-Bernal7, Anh T. Le7, Nisha Nanda8, Michael C. Cox8, Robert C. Doebele7

LOXO ONCOLOGY

At Loxo Oncology, we are motivated by our goal of improving the lives of people living with cancer. Our team members choose to be part of Loxo Oncology because we share this passion and believe in our values. If our passion and values resonate with you, Loxo Oncology may be in your DNA. Learn more about current opportunities with Loxo Oncology. LIFE AT LOXO ONCOLOGY Josh Ballard Research Fellow, Biochemistry. "Loxo Oncology at Lilly leverages the capabilities and breadth of experience from Lilly while maintaining a nimble, patient-centered biotech mindset. The culture is anchored in significant collaboration and real-time, patient-centric decision making. For people who like working in an environment that CAREER OPPORTUNITIES Loxo Oncology, Inc. (Loxo) currently anticipates that the base salary for this position could range from between $135,300 to $198,516 and will depend, in part, on the successful candidate’s qualifications for the role, including education and experience. LOXO-305 (BTK INHIBITOR) Pirtobrutinib (LOXO-305) Pirtobrutinib is an investigational, oral, highly-selective non-covalent Bruton’s tyrosine kinase (BTK) inhibitor. BTK plays a key role in the B-cell antigen receptor signaling pathway, which is required for the development, activation and survival of normal white blood cells, known as B-cells, and

malignant B-cells.

MANAGEMENT TEAM

The Loxo Oncology management team is motivated by one goal: to dramatically improve the lives of people living with cancer. CAREER OPPORTUNITIES Patients are at the heart of everything we do at Loxo Oncology, and we continue to be motivated by our goal of improving the lives of people

living with cancer.

PRECLINICAL CHARACTERIZATION OF LOXO-338, A NOVEL, ORAL Preclinical characterization of LOXO-338, a novel, oral and selective BCL2 inhibitor Presented at: AACR Annual Meeting 2021 Date: April 10,

2021

PRE-CLINICAL CHARACTERIZATION OF POTENT AND SELECTIVE NEXT Crystal structure of selpercatinib (gray) bound to RET V804M (V804M gatekeeper residue shown in green). Selpercatinib is a potent inhibitor of RET V804M. RESULTS FROM THE FIRST-IN-HUMAN, PROOF-OF-CONCEPT PHASE 1LOXO 305 PDFLOXO 305 TRIALLATE BREAKING ABSTRACT LOXO 305LOXO 305 CLINICAL TRIALSLOXO 305 SIDE EFFECTSLOXO 305 STRUCTURE Presented at: 2019 ASH Annual Meeting Date: December 8, 2019. Results from the First-in-Human, Proof-of-Concept . Phase 1 BRUIN Trial in Pretreated B -Cell Malignancies for LOXO- 305, a Next- Generation, A PEDIATRIC PHASE 1 STUDY OF LAROTRECTINIB, A HIGHLY Pharmacokinetics 9 Concentration-time AUC 0–24 in patients treated with 80–125 mg/m2 BID Laetsch, 10510 0 1 10 100 tinib g/mL) 1000 3 6 Time (hours) 9 12 Adults (100 mg

LOXO ONCOLOGY

At Loxo Oncology, we are motivated by our goal of improving the lives of people living with cancer. Our team members choose to be part of Loxo Oncology because we share this passion and believe in our values. If our passion and values resonate with you, Loxo Oncology may be in your DNA. Learn more about current opportunities with Loxo Oncology. LIFE AT LOXO ONCOLOGY Josh Ballard Research Fellow, Biochemistry. "Loxo Oncology at Lilly leverages the capabilities and breadth of experience from Lilly while maintaining a nimble, patient-centered biotech mindset. The culture is anchored in significant collaboration and real-time, patient-centric decision making. For people who like working in an environment that CAREER OPPORTUNITIES Loxo Oncology, Inc. (Loxo) currently anticipates that the base salary for this position could range from between $135,300 to $198,516 and will depend, in part, on the successful candidate’s qualifications for the role, including education and experience. LOXO-305 (BTK INHIBITOR) Pirtobrutinib (LOXO-305) Pirtobrutinib is an investigational, oral, highly-selective non-covalent Bruton’s tyrosine kinase (BTK) inhibitor. BTK plays a key role in the B-cell antigen receptor signaling pathway, which is required for the development, activation and survival of normal white blood cells, known as B-cells, and

malignant B-cells.

MANAGEMENT TEAM

The Loxo Oncology management team is motivated by one goal: to dramatically improve the lives of people living with cancer. CAREER OPPORTUNITIES Patients are at the heart of everything we do at Loxo Oncology, and we continue to be motivated by our goal of improving the lives of people

living with cancer.

PRECLINICAL CHARACTERIZATION OF LOXO-338, A NOVEL, ORAL Preclinical characterization of LOXO-338, a novel, oral and selective BCL2 inhibitor Presented at: AACR Annual Meeting 2021 Date: April 10,

2021

PRE-CLINICAL CHARACTERIZATION OF POTENT AND SELECTIVE NEXT Crystal structure of selpercatinib (gray) bound to RET V804M (V804M gatekeeper residue shown in green). Selpercatinib is a potent inhibitor of RET V804M. RESULTS FROM THE FIRST-IN-HUMAN, PROOF-OF-CONCEPT PHASE 1LOXO 305 PDFLOXO 305 TRIALLATE BREAKING ABSTRACT LOXO 305LOXO 305 CLINICAL TRIALSLOXO 305 SIDE EFFECTSLOXO 305 STRUCTURE Presented at: 2019 ASH Annual Meeting Date: December 8, 2019. Results from the First-in-Human, Proof-of-Concept . Phase 1 BRUIN Trial in Pretreated B -Cell Malignancies for LOXO- 305, a Next- Generation, A PEDIATRIC PHASE 1 STUDY OF LAROTRECTINIB, A HIGHLY Pharmacokinetics 9 Concentration-time AUC 0–24 in patients treated with 80–125 mg/m2 BID Laetsch, 10510 0 1 10 100 tinib g/mL) 1000 3 6 Time (hours) 9 12 Adults (100 mg PARTNERS | LOXO ONCOLOGY Loxo Oncology at Lilly supports third-party research that is aimed at furthering scientific knowledge and understanding in oncology. Loxo Oncology at Lilly will assess proposals for providing study drug and/or financial support for Investigator-Initiated Research based on scientific merit and strategic fit with our areas of research

interest.

PIPELINE | LOXO ONCOLOGY Pipeline Overview. Loxo Oncology at Lilly seeks to discover and develop a broad pipeline of treatments with the potential to make a meaningful difference for people living with cancer. The safety and efficacy of the agents and uses under investigation have not been

established.

PIPELINE | LOXO ONCOLOGY Pipeline Overview. Loxo Oncology at Lilly seeks to discover and develop a broad pipeline of treatments with the potential to make a meaningful difference for people living with cancer. LY3484356 | LOXO ONCOLOGY LY3484356 is an investigational, oral selective estrogen receptor degrader (SERD) with pure antagonistic properties. The estrogen receptor (ER) is the key therapeutic target for patients with

ER+/HER2-

PRE-CLINICAL CHARACTERIZATION OF POTENT AND SELECTIVE NEXT Crystal structure of selpercatinib (gray) bound to RET V804M (V804M gatekeeper residue shown in green). Selpercatinib is a potent inhibitor of RET V804M. A FIRST-IN-HUMAN PHASE 1A/B TRIAL OF LY3484356, AN ORAL Presented at: ASCO Annual Meeting 2021 Date: June 4, 2021. A first-in-human phase 1a/b trial of LY3484356, an oral selective estrogen receptor (ER) degrader (SERD) in RESULTS FROM THE FIRST-IN-HUMAN, PROOF-OF-CONCEPT PHASE 1 Presented at: 2019 ASH Annual Meeting Date: December 8, 2019. Results from the First-in-Human, Proof-of-Concept . Phase 1 BRUIN Trial in Pretreated B -Cell Malignancies for LOXO- 305, a Next- Generation, CLINICAL ACTIVITY OF LOXO-292, A HIGHLY SELECTIVE RET Clinical Activity of LOXO-292, a Highly Selective RET Inhibitor, in Patients with RET Fusion+ Non-Small Cell Lung Cancer An Update from ASCO 2018 Geoffrey R. Oxnard, Vivek Subbiah, Keunchil Park, Todd M. Bauer, Lori J. Wirth, Vamsidhar

TERMS OF USE

Such statements may be indicated by the use of words such as “anticipate,” “estimate,” “expect,” “project,” “intend,” “plan,” “believe,” and other terms of similar meaning appearing in discussions of future operating or financial performance. Such statements are based on company management’s current expectations CLINICAL SAFETY AND ACTIVITY FROM A PHASE 1 STUDY OF LOXO Clinical safety and activity from a Phase 1 study of LOXO-101, a selective TRKA/B/C inhibitor, in solid-tumor patients with NTRK gene fusions David S. Hong1, Anna F. Farago2,Marcia S. Brose3, Howard A. Burris, III4, Afshin Dowlati5, Todd M. Bauer4, Matthew Taylor6, Alice T. Shaw2,Adriana Estrada-Bernal7, Anh T. Le7, Nisha Nanda8, Michael C. Cox8, Robert C. Doebele7

* About Us

* Company Overview

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* Partners

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LOXO ONCOLOGY AT LILLY DEVELOPMENT APPROACH CAREER OPPORTUNITIES IS LOXO ONCOLOGY IN YOUR DNA? At Loxo Oncology, we are motivated by our goal of improving the lives of people living with cancer. Our team members choose to be part of Loxo Oncology because we share this passion and believe in our values. If our passion and values resonate with you, Loxo Oncology may be in

your DNA.

Learn more about current opportunities with Loxo Oncology.

Join Our Team

CAREER OPPORTUNITIES IS LOXO ONCOLOGY IN YOUR DNA? At Loxo Oncology, we are motivated by our goal of improving the lives of people living with cancer. Our team members choose to be part of Loxo Oncology because we share this passion and believe in our values. If our passion and values resonate with you, Loxo Oncology may be in

your DNA.

Learn more about current opportunities with Loxo Oncology.

Join Our Team

ABOUT US

* Company Overview

* Leadership Team

PROGRAMS

* Pipeline

* Pirtobrutinib (LOXO-305) * LY3484356 (Oral SERD) * Publications & Presentations * Access to Investigational Agents PATIENTS & CAREGIVERS

PARTNERS

CAREERS

* Life at Loxo

* Careers

CONTACT US

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