> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/divarasib-1a5e0f51-591c-4413-a16a-669de4706ffe
> Record changed: 2026-10-13

# Divarasib

Highest phase reached

Phase 2

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095236)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095236)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 2

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095236)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095236)

**Drug name**

Divarasib

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095236)

**Molecular weight**

622.07

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095236)

**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

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095236)

### Other names (21)

- 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

## Identifiers

**CAS registry numbers**

- 2417987-45-0

**ChEMBL ID**

CHEMBL5095236

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095236)

**InChIKey**

ZRBPIAWWRPFDPY-IRXDYDNUSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095236)

**PubChem compound IDs**

- 146624881

**FDA ingredient codes (UNII)**

- E6S21PVT91

## Regulatory information

### Other regulatory facts

**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

### Drug classification

**Pharmacology name**

divarasib

**Type**

Synthetic organic

**Drug name stem**

\-rasib

### Mechanisms of action (2)

- **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

### Investigated indications (2)

- **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

### Open Targets indications (7)

- **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

### Trial references (4)

- NCT03178552  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03178552)
- NCT04302025  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04302025)
- NCT05789082  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05789082)
- NCT04589845  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04589845)

## Chemical properties

**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

## Evidence counts

**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)](https://trialight.com/data/trial/a-study-evaluating-the-safety-and-efficacy-of-targeted-dd62fe2e-2b36-4ddc-82bc-7f1549d780cc.md)
- [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](https://trialight.com/data/trial/a-study-evaluating-the-safety-activity-and-pharmacokinetics-4c3cad97-2547-429f-86a8-9db6b79a2a04.md)
- 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](https://trialight.com/data/condition/non-small-cell-lung-carcinoma-a86c1d60-523f-5ea7-a5e1-39ed4a2296f8.md) Phase 2

---

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