Sotorasib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2021
- First approval year
- 2021
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Sotorasib
- Molecular weight
- 560.61
- Structure (SMILES)
- C=CC(=O)N1CCN(c2nc(=O)n(-c3c(C)ccnc3C(C)C)c3nc(-c4c(O)cccc4F)c(F)cc23)[C@@H](C)C1
- lumakras
- Lumakras
- lumykras
- Lumykras
- (R)-38
- (S)-AMG-510
- amg 510
- AMG 510
- AMG-510
- amg510
- AMG510
- ct amg510amg 510amg510
- CT-AMG510AMG-510AMG510
- kras g12c inhibitor 9
- Kras g12c inhibitor 9
- KRAS G12C INHIBITOR 9
- kras mutant targeting amg 510
- Kras mutant-targeting amg 510
- KRAS MUTANT-TARGETING AMG 510
- lumakras
- LUMAKRAS
- lumykras
- LUMYKRAS
- r 38
- s amg 510
- sotorasib
- Sotorasib
- SOTORASIB
- SOTORASIB (AMG510) RACEMATE
And 14 more, listed on the interactive page.
- ATC classification codes
- L01XX73
Sources for recorded values
- CAS registry numbers
- 2296729-00-3
- ChEMBL ID
- CHEMBL4535757
- InChIKey
- NXQKSXLFSAEQCZ-SFHVURJKSA-N
- PubChem compound IDs
- 137278711
- RxNorm IDs (RxCUI)
- 2550714
- FDA ingredient codes (UNII)
- 2B2VM6UC8G
- Applicant
- AMGEN INC
- Approval date
- 28 May 2021
- Application number
- NDA214665
- Status
- Authorised
- Status date
- 6 Jan 2022
- Authorisation date
- 6 Jan 2022
- Approved indications
- Lumykras as monotherapy is indicated for the treatment of adults with advanced non-small cell lung cancer (NSCLC) with KRAS G12C mutation and who have progressed after at least one prior line of systemic therapy.
- Product number
- EMEA/H/C/005522
- Authorisation holder
- Amgen Europe B.V.
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- Yes
- Additional monitoring
- Yes
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Carcinoma, Non-Small-Cell Lung
European medicines record
- Patents
- 6
- Designations
- 8
- Earliest recorded loss of exclusivity
- 15 Sept 2040
- First in class
- Yes
- Fast track
- Yes
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- Yes
- Availability
- Prescription only
- Pharmacology name
- sotorasib
- Type
- Synthetic organic
- Drug name stem
- -rasib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- KRAS
- Gene symbol
- KRAS
- Protein identifier
- P01116
- Median affinity
- 10.39
- Affinity units
- pKi
- Mechanism
- GTPase KRas inhibitor
- Action type
- Inhibitor
- Target
- GTPase KRas
- Protein identifier
- P01116
Open Targets mechanisms
- Mechanism
- GTPase KRas inhibitor
- Action type
- Inhibitor
- Target
- GTPase KRas
DrugCentral mechanisms
- Action type
- Inhibitor
- Gene symbol
- KRAS
- Protein identifier
- P01116
- Organism
- Homo sapiens
- Target development level
- Chemical evidence
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Ovarian Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001075
- Subject identifier
- D010051
- Condition
- Liver Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001421
- Subject identifier
- D008107
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0002618
- Subject identifier
- D010190
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 4
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0005575
- Subject identifier
- D015179
- Condition
- Lung Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0008903
- Subject identifier
- D008175
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0001421
- Highest recorded phase
- 1
- Condition identifier
- EFO_0003060
- Condition identifier
- EFO_0003833
- Highest recorded phase
- 1
- Condition identifier
- EFO_1000044
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0003060
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005008
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005070
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005192
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005233
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005575
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0006047
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0007254
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0008170
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0008903
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0009831
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0011962
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0021211
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0021350
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0056806
- Highest recorded phase
- 2
- Event
- non-small cell lung cancer
- Reports
- 12
- Reporting signal score
- 69.6457
- Event
- non-small cell lung cancer metastatic
- Reports
- 2
- Reporting signal score
- 12.0295
- NCT03600883
- NCT04092673
- NCT04185883
- NCT04380753
- NCT05638295
- NCT04303780
- NCT04625647
- NCT04720976
- NCT04933695
- NCT04959981
- NCT05054725
- NCT05180422
- NCT05311709
- NCT05313009
- NCT05374538
- NCT05398094
- NCT05400577
- NCT05451056
- NCT05480865
- NCT05631249
- NCT05815173
- NCT05815186
- NCT06068153
- NCT06249282
- NCT06333678
And 6 more, listed on the interactive page.
- Dose
- 960 mg
- Route
- Orally
- How often
- Once daily
- Swallow tablets whole
- Take with or without food
- Hydrogen bond acceptors
- 8
- Hydrogen bond donors
- 1
- Polar surface area
- 104.45
- Calculated partition coefficient (ALogP)
- 4.48
- Calculated partition coefficient (XLogP)
- 4
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 1
- Rotatable bonds
- 5
- Heavy atoms
- 41
- Molecular formula
- C30H30F2N6O3
- Monoisotopic mass
- 560.23474516
- Natural product
- No
- 55513-488
- 55513-504
- 55513-512
- Recorded assays
- 302
- Active assays
- 49
Active assay types
- Confirmatory
- Antineoplastic Agents
These details could not be displayed.
Related records
Trials (68)
- A 2-part Phase 1/2 Open-label Trial on ODM-212
- A Clinical Trial to Evaluate Bioavailability and Effect of Food for Sotorasib in Healthy Participants
- A First-in-Human (FIH) Study to Evaluate the Safety and Tolerability of VVD-159642 in Participants With Advanced Solid Tumors
- A Phase 1/2, Study Evaluating the Safety, Tolerability, PK, and Efficacy of Sotorasib (AMG 510) in Subjects With Solid Tumors With a Specific KRAS Mutation (CodeBreaK 100)
- A Phase 2 Basket Trial in Which Patients With Advanced Solid Tumors Carrying the KRAS G12C mUtation Receive Treatment With a Combination of Sotorasib and Panitumumab
- A Phase I/II Study of AMG 510 in Combination With MVASI in Patients With Advanced, Unresectable or Metastatic KRAS G12C Mutant NSCLC With Asymptomatic Brain Metastasis
- A Phase II Study of Neoadjuvant Sotorasib in Combination With Cisplatin or Carboplatin and Pemetrexed for Surgically Resectable Stage IIA-IIIB Non-Squamous Non-Small Cell Lung Cancer With a KRAS p.G12C Mutation
- A Rollover Study Evaluating Sotorasib With or Without Panitumumab in Participants With KRAS p.G12C Mutation
- A Study Comparing Sotorasib With Durvalumab in People With Non-Small Cell Lung Cancer (NSCLC)
- A Study Evaluating Sotorasib Platinum Doublet Combination Versus Pembrolizumab Platinum Doublet Combination as a Front-Line Therapy in Participants With Stage IV or Advanced Stage IIIB/C Nonsquamous Non-Small Cell Lung Cancers (CodeBreaK 202)
- A Study Evaluating the Efficacy and Safety of Divarasib Versus Sotorasib or Adagrasib in Participants With Previously Treated KRAS G12C-positive Advanced or Metastatic Non-Small Cell Lung Cancer
- A Study in Healthy Volunteers to Compare the Pharmacokinetics of Sotorasib Administered as 1 or 2 Tablets
- A Study of Anti-Cancer Therapies Targeting the MAPK Pathway in Patients With Advanced NSCLC
- A Study of Sotorasib (AMG 510) in Participants With Stage IV NSCLC Whose Tumors Harbor a KRAS p.G12C Mutation in Need of First-line Treatment
- A Study of Sotorasib in People With Brain Tumors
- A Study of Sotorasib in People With Non-Small Cell Lung Cancer
- A Study of the Absorption, Metabolism, and Excretion of [14C]-AMG 510 Following a Single Oral Dose in Healthy Male Subjects
- A Study to Assess the Effect of Food on the Pharmacokinetics (PK) of AMG 510 in Healthy Participants
- A Study to Compare the Pharmacokinetics of Two Different Tablets of Sotorasib in Healthy Participants
- A Study to Evaluate the Drug-drug Interaction Effect of Itraconazole on the Pharmacokinetics (PK) of AMG 510 in Healthy Participants
Approved for (2)
- Neoplasm
- Non-small cell lung carcinoma
In development for (7)
- Brain neoplasm Phase 1
- Colorectal cancer Phase 3
- Exocrine pancreatic carcinoma Phase 1
- Liver disorder Phase 1
- Lung cancer Phase 2
- Ovarian carcinoma Phase 2
- Pancreatic adenocarcinoma Phase 2
Targets (1)
- KRAS GTPase KRas inhibitor