Divarasib
Highest phase reached
Phase 2
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Phase 2
- Drug type
- Small molecule
- Drug name
- Divarasib
- Molecular weight
- 622.07
- Structure (SMILES)
- C=CC(=O)N1CCN(c2nc(OC[C@@H]3CCCN3C)nc3c(F)c(-c4nc(N)cc(C)c4C(F)(F)F)c(Cl)cc23)[C@@H](C)C1
- 1 3s 4 7r 7 6 amino 4 methyl 3 trifluoromethyl 2 pyridinyl 6 chloro 8 fluoro 2 2s 1 methyl 2 pyrrolidinyl methoxy 4 quinazolinyl 3 methyl 1 piperazinyl 2 propen 1 one
- 1-[(3S)-4-[(7R)-7-[6-Amino-4-methyl-3-(trifluoromethyl)-2-pyridinyl]-6-chloro-8-fluoro-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]-4-quinazolinyl]-3-methyl-1-piperazinyl]-2-propen-1-one
- divarasib
- Divarasib
- divarasib [INN]
- DIVARASIB [USAN]
- Divarasib [WHO-DD]
- divarasib inn
- divarasib usan
- divarasib who dd
- gdc 6036
- Gdc 6036
- GDC-6036
- rg 6330
- RG-6330
- rg6330
- RG6330
- ro 7435846
- RO-7435846
- ro7435846
- RO7435846
- CAS registry numbers
- 2417987-45-0
- ChEMBL ID
- CHEMBL5095236
- InChIKey
- ZRBPIAWWRPFDPY-IRXDYDNUSA-N
- PubChem compound IDs
- 146624881
- FDA ingredient codes (UNII)
- E6S21PVT91
- Patents
- 0
- Designations
- 1
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Pharmacology name
- divarasib
- Type
- Synthetic organic
- Drug name stem
- -rasib
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- KRAS
- Gene symbol
- KRAS
- Protein identifier
- P01116
- Median affinity
- 8
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- KRAS
- Gene symbol
- KRAS
- Protein identifier
- P01116
- Median affinity
- 12.62
- Affinity units
- pKd
- Condition
- Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition identifier
- EFO_0000616
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0002714
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005070
- Condition identifier
- MONDO_0005233
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005575
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0006130
- Highest recorded phase
- 2
- NCT03178552
- NCT04302025
- NCT05789082
- NCT04589845
- Hydrogen bond acceptors
- 8
- Hydrogen bond donors
- 1
- Polar surface area
- 100.71
- Calculated partition coefficient (ALogP)
- 5.09
- Calculated partition coefficient (XLogP)
- 5.4
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 2
- Rotatable bonds
- 6
- Heavy atoms
- 43
- Molecular formula
- C29H32ClF4N7O2
- Monoisotopic mass
- 621.2242136
- Natural product
- No
- Recorded assays
- 68
- Active assays
- 4
Active assay types
- Confirmatory
Related records
Trials (15)
- A Clinical Trial to Investigate the Clinical Drug-Drug Interaction of Divarasib With Probe Substrates of P-Glycoprotein and Breast Cancer Resistance Protein in Healthy Participants
- A Rollover Study for Participants Previously Enrolled in a Genentech and/or F. Hoffman-La Roche Sponsored Study
- A Study Evaluating the Efficacy and Safety of Divarasib and Pembrolizumab Versus Pembrolizumab and Pemetrexed and Carboplatin or Cisplatin in Participants With Previously Untreated, KRAS G12C-Mutated, Advanced or Metastatic Non-Squamous Non-Small Cell Lung Cancer
- 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 Evaluating the Safety and Efficacy of Targeted Therapies in Subpopulations of Patients With Metastatic Colorectal Cancer (INTRINSIC)
- A Study Evaluating the Safety, Activity, and Pharmacokinetics of Divarasib as a Single Agent or in Combination With Other Anti-Cancer Therapies in Participants With Previously Untreated Advanced or Metastatic Non-Small Cell Lung Cancer With a KRAS G12C Mutation
- A Study of Multiple Therapies in Biomarker-selected Participants With Resectable Stages IB-III Non-small Cell Lung Cancer (NSCLC)
- A Study to Determine the Effect of Itraconazole on the Pharmacokinetics of Divarasib in Healthy Participants
- A Study to Evaluate the Effect of Rifampin on the Pharmacokinetics of Divarasib in Healthy Participants
- A Study to Evaluate the Efficacy and Safety of Divarasib Compared With Investigator's Choice of Immunotherapy or Observation in Participants With Resected Stage II-III KRAS G12C-Positive Non-Small Cell Lung Cancer (NSCLC)
- A Study to Evaluate the Efficacy and Safety of Multiple Targeted Therapies as Treatments for Participants With Non-Small Cell Lung Cancer (NSCLC)
- A Study to Evaluate the Pharmacokinetics of Divarasib in Healthy Participants and Participants With Impaired Hepatic Function
- A Study to Evaluate the Safety, Pharmacokinetics, and Activity of GDC-6036 Alone or in Combination in Participants With Advanced or Metastatic Solid Tumors With a KRAS G12C Mutation
- An Expanded Access Program to Provide Divarasib to Participants With Previously Treated KRAS G12c-Positive Advanced or Metastatic Non-Small Cell Lung Cancer
- Tumor-agnostic Precision Immuno-oncology and Somatic Targeting Rational for You (TAPISTRY) Platform Study
In development for (2)
- Neoplasm Phase 2
- Non-small cell lung carcinoma Phase 2