Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
LY3537982 · 8 trials · 10 indications
Dose Optimization and Safety Lead-In Part B: Number of Participants with a TEAE
PFS per Response Evaluation Criteria in Solid Tumors (RECIST) v1.1 by blinded independent central review (BICR)
PK: Cmax of LY3537982
PK: AUC of LY3537982
Part 1: PK: Cmax of LY3537982
Part 1: PK: AUC\[0-inf\] of LY3537982
Part 1: PK: AUClast of LY3537982
Part 1: PK: AUC\[0-inf\] of Digoxin
Part 1: PK: AUC\[0-inf\] of Rosuvastatin
Part 2: PK: AUC\[0-inf\] of LY3537982
Part 2: PK: AUC\[0-inf\] of Midazolam
Part 2: PK: AUC\[0-inf\] of 1'-Hydroxymidazolam
PK: Feur
PK: Fefeces
PK: Feair
PK: F of LY3537982
PK: Cmax of LY3537982 administered with or without itraconazole
PK: AUC\[0-inf\] of LY3537982 administered with or without itraconazole
PK: AUClast of LY3537982 administered with or without itraconazole
PK: AUC\[0-inf\] of LY3537982 administered with or without carbamazepine
PK: AUC(0-inf)
PK: Cmax of LY3537982
Measured by the number of patients with dose-limiting toxicities (DLTs)
Measured by the number of patients with dose-limiting toxicities (DLTs)
Measured by TEAEs
| Arm | Type | Description |
|---|---|---|
| Dose Optimization: LY3537982 Dose Level 1 plus Pembrolizumab | EXPERIMENTAL | LY3537982 Dose level 1 administered orally in combination with pembrolizumab administered intravenously (IV) in 21-day cycles. Participants may continue to receive treatment until discontinuation criteria are met. |
| Dose Optimization: LY3537982 Dose Level 2 plus Pembrolizumab | EXPERIMENTAL | LY3537982 Dose level 2 administered orally in combination with pembrolizumab administered IV in 21-day cycles. Participants may continue to receive treatment until discontinuation criteria are met. |
| Safety Lead In: LY3537982 plus Pembrolizumab, Pemetrexed and Platinum | EXPERIMENTAL | LY3537982 administered orally in combination with pembrolizumab, pemetrexed, and platinum (cisplatin or carboplatin) administered IV in 21-day cycles. Participants may continue to receive treatment until discontinuation criteria are met. |
| Part A: LY3537982 plus Pembrolizumab | EXPERIMENTAL | LY3537982 administered orally in combination with pembrolizumab administered IV in 21-day cycles. Participants may continue to receive treatment until discontinuation criteria are met. |
| Part A: Placebo plus Pembrolizumab | PLACEBO_COMPARATOR | Placebo administered orally in combination with pembrolizumab administered IV in 21-day cycles. Participants may continue to receive treatment until discontinuation criteria are met. |
| Part B: LY3537982 plus Pembrolizumab, Pemetrexed, and Platinum | EXPERIMENTAL | LY3537982 administered orally in combination with pembrolizumab, pemetrexed, and platinum (cisplatin or carboplatin) administered IV in 21-day cycles. Participants may continue to receive treatment until discontinuation criteria are met. |
| Part B: Placebo plus Pembrolizumab, Pemetrexed, and Platinum | PLACEBO_COMPARATOR | Placebo administered orally in combination with pembrolizumab, pemetrexed, and platinum (cisplatin or carboplatin) administered IV in 21-day cycles. Participants may continue to receive treatment until discontinuation criteria are met. |
| Part C: LY3537982 plus Pembrolizumab | EXPERIMENTAL | LY3537982 administered orally in combination with pembrolizumab administered IV in 21-day cycles. Participants may continue to receive treatment until discontinuation criteria are met. |
| LY3537982 (Normal renal function) | EXPERIMENTAL | LY3537982 administered orally. |
| LY3537982 (Severe renal impairment) | EXPERIMENTAL | LY3537982 administered orally. |
| LY3537982 (Moderate renal impairment) | EXPERIMENTAL | LY3537982 administered orally. |
| LY3537982 | EXPERIMENTAL | LY3537982 administered orally. |
| LY3537982 + Digoxin & Rosuvastatin (Part 1) | EXPERIMENTAL | Single oral doses of digoxin and rosuvastatin with or without multiple doses of LY3537982 administered orally |
| LY3537982 + Midazolam (Part 2) | EXPERIMENTAL | Single doses of midazolam administered either orally or intravenously (IV) with or without multiple doses of LY3537982 administered orally |
| [¹⁴C]-LY3537982 (Part 1) | EXPERIMENTAL | Single dose of \[¹⁴C\]-LY3537982 administered orally. |
| [¹⁴C]-LY3537982 + LY3537982 (Part 2) | EXPERIMENTAL | Single dose of LY3537982 administered orally followed by \[¹⁴C\]-LY3537982 administered intravenously (IV). |
| LY3537982 + Itraconazole (Part 1) | EXPERIMENTAL | LY3537982 administered orally alone followed by LY3537982 administered in combination with itraconazole orally. |
| LY3537982 + Carbamazepine (Part 2) | EXPERIMENTAL | LY3537982 administered orally alone followed by LY3537982 administered in combination with carbamazepine orally. |
| LY3537982 (High-Fat Meal) | EXPERIMENTAL | LY3537982 administered orally under fasting conditions in one study period and under fed conditions (i.e., a standard high-fat meal) in the other study period. |
| LY3537982 (Low-Fat Meal) | EXPERIMENTAL | LY3537982 administered orally under fasting conditions in one study period and under fed conditions (i.e., a standard low-fat meal) in the other study period. |
| LY3537982 (Dose Escalation) | EXPERIMENTAL | LY3537982 administered orally. |
| LY3537982 (Dose Expansion) | EXPERIMENTAL | LY3537982 administered orally either alone or with another investigational agent. |
| LY3537982 (Dose Optimization) | EXPERIMENTAL | LY3537982 administered orally either alone or with another investigational agent |
| Name | Type | Description |
|---|---|---|
| LY3537982 | DRUG | Administered orally. |
| Pembrolizumab | DRUG | Administered IV. |
| Placebo | DRUG | Administered orally. |
| Cisplatin | DRUG | Administered IV. |
| Carboplatin | DRUG | Administered IV. |
| Pemetrexed | DRUG | Administered IV. |
| Digoxin | DRUG | Administered orally |
| Rosuvastatin | DRUG | Administered orally |
| Midazolam | DRUG | Administered orally |
| [¹⁴C]-LY3537982 | DRUG | Administered orally. |
| Itraconazole | DRUG | Administered orally. |
| Carbamazepine | DRUG | Administered orally. |
| Cetuximab | DRUG | Intravenous |
Inclusion Criteria: * Histologically or cytologically confirmed NSCLC with Stage IIIB-IIIC or Stage IV disease, not suitable for curative intent radical surgery or radiation therapy. * Part B and Safety Lead-In Part B: the histology of the tumor must be predominantly non-squamous (in line with peme...
LY3537982 is an investigational small molecule being studied for advanced solid tumors, carcinoma, non-small-cell lung cancer, and renal insufficiency. It is being evaluated in patients with KRAS G12C mutations, including those with non-small-cell lung cancer, colorectal, endometrial, ovarian, pancreatic, and biliary tract neoplasms.
LY3537982 targets KRAS G12C, a specific genetic mutation found in certain cancers. By targeting this mutant form of the KRAS protein, the drug is designed to interfere with cancer cell growth driven by this mutation.
LY3537982 is being developed by Eli Lilly and Company, a pharmaceutical company traded on the NYSE under the ticker LLY.
LY3537982 is in clinical development. It has been studied in Phase 1 trials for advanced solid tumors and renal insufficiency, and is currently being evaluated in a Phase 3 trial for first-line advanced KRAS G12C-mutant non-small cell lung cancer.
LY3537982 is being studied in several trials. NCT04956640 is a Phase 1 study in cancer patients with KRAS G12C mutations. NCT06119581 is a Phase 3 trial combining LY3537982 with pembrolizumab and chemotherapy in non-small cell lung cancer. NCT06235983 and NCT07137689 are completed Phase 1 studies in Chinese participants and those with kidney problems.
Yes, LY3537982 is also known as olomorasib. In clinical trial NCT06119581, the drug is referred to as olomorasib (LY3537982), confirming that both names refer to the same investigational agent.