Last reviewed · How we verify
Lumakras (SOTORASIB)
Lumakras works by covalently binding to the KRAS G12C mutation, thereby blocking the protein's ability to promote cancer cell growth.
Lumakras (Sotorasib) is a small molecule therapy developed by Amgen Inc, targeting the GTPase KRas protein. It is approved for the treatment of KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer. Lumakras is a patented medication with no generic manufacturers available. The drug was approved by the FDA in 2021 and is currently owned by Amgen Inc. Key safety considerations include potential liver enzyme elevations and gastrointestinal toxicities.
At a glance
| Generic name | SOTORASIB |
|---|---|
| Sponsor | Amgen |
| Target | GTPase KRas |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2021 |
| Annual revenue | 300 |
Mechanism of action
Sotorasib is an inhibitor of KRASG12C, tumor-restricted, mutant-oncogenic form of the RAS GTPase, KRAS. Sotorasib forms an irreversible, covalent bond with the unique cysteine of KRASG12C, locking the protein in an inactive state that prevents downstream signaling without affecting wild-type KRAS. Sotorasib blocked KRAS signaling, inhibited cell growth, and promoted apoptosis only in KRAS G12C tumor cell lines. Sotorasib inhibited KRASG12C in vitro and in vivo with minimal detectable off-target activity. In mouse tumor xenograft models, sotorasib-treatment led to tumor regressions and prolonged survival, and was associated with anti-tumor immunity in KRAS G12C models.
Approved indications
- KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer
Common side effects
- Diarrhea
- Musculoskeletal pain
- Nausea
- Fatigue
- Hepatotoxicity
- Cough
- Decreased lymphocytes
- Decreased hemoglobin
- Increased aspartate aminotransferase
- Increased alanine aminotransferase
- Decreased calcium
- Increased alkaline phosphatase
Key clinical trials
- Targeted Therapy Directed by Genetic Testing in Treating Patients With Locally Advanced or Advanced Solid Tumors, The ComboMATCH Screening Trial (PHASE2)
- Sotorasib in Combination With Trastuzumab Deruxtecan for the Treatment of Locally Advanced and Metastatic Non-small Cell Lung Cancer With a KRAS G12C Mutation (PHASE1,PHASE2)
- Testing the Use of AMG 510 (Sotorasib) and Panitumumab as a Targeted Treatment for KRAS G12C Mutant Solid Tumor Cancers (A ComboMATCH Treatment Trial) (PHASE2)
- Study to Compare AMG 510 "Proposed INN Sotorasib" With Docetaxel in Non Small Cell Lung Cancer (NSCLC) (CodeBreak 200). (PHASE3)
- A Rollover Study Evaluating Sotorasib With or Without Panitumumab in Participants With KRAS p.G12C Mutation (PHASE2)
- A Study of Sotorasib in People With Non-Small Cell Lung Cancer (PHASE2)
- AMG 193 Alone or in Combination With Other Therapies in Subjects With Advanced Thoracic Tumors With Homozygous MTAP-deletion (Master Protocol) (MTAPESTRY 104). (PHASE1)
- AMG 510 Ethnic Sensitivity Study (CodeBreaK 105). (PHASE1)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
| SEC EDGAR | Revenue + earnings |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Lumakras CI brief — competitive landscape report
- Lumakras updates RSS · CI watch RSS
- Amgen portfolio CI