> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/setidegrasib-947fc0f8-4ff5-4a70-8577-baf5799fb8ef
> Record changed: 2026-10-13

# Setidegrasib

Highest phase reached

Phase 2

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068173)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068173)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 2

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068173)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068173)

**Drug name**

Setidegrasib

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068173)

**Structure (SMILES)**

c1n\[nH\]c2cc(c(C)c(c21)-c3c(OCc4ccc(cc4)-c5cn(\[C@H\](C(=O)N6C\[C@@H\](C\[C@H\]6C(N\[C@H\](c7ccc(-c8c(ncs8)C)cc7)CO)=O)O)C(C)C)nn5)c9c(c(N%10\[C@@\]%11(CN\[C@@\](\[H\])(C%11)C%10)\[H\])nc(n9)OC%12CCOCC%12)cc3C%13CC%13)F

Source: [gsrs.ncats.nih.gov](https://gsrs.ncats.nih.gov/ginas/app/beta/substances/3NQ4ME292X)

### Other names (8)

- 2 pyrrolidinecarboxamide 1 2s 2 4 4 6 cyclopropyl 4 1s 4s 2 5 diazabicyclo 2 2 1 hept 2 yl 7 6 fluoro 5 methyl 1h indazol 4 yl 2 tetrahydro 2h pyran 4 yl oxy 8 quinazolinyl oxy methyl phenyl 1h 1 2 3 triazol 1 yl 3 methyl 1 oxobutyl 4 hydroxy n 1r 2 hydroxy 1 4 4 methyl 5 thiazolyl phenyl ethyl 2s 4r
- 2-Pyrrolidinecarboxamide, 1-\[(2S)-2-\[4-\[4-\[\[\[6-cyclopropyl-4-(1S,4S)-2,5-diazabicyclo\[2.2.1\]hept-2-yl-7-(6-fluoro-5-methyl-1H-indazol-4-yl)-2-\[(tetrahydro-2H-pyran-4-yl)oxy\]-8-quinazolinyl\]oxy\]methyl\]phenyl\]-1H-1,2,3-triazol-1-yl\]-3-methyl-1-oxobutyl\]-4-hydroxy-N-\[(1R)-2-hydroxy-1-\[4-(4-methyl-5-thiazolyl)phenyl\]ethyl\]-, (2S,4R)-
- setidegrasib
- Setidegrasib
- setidegrasib \[INN\]
- Setidegrasib \[WHO-DD\]
- setidegrasib inn
- setidegrasib who dd

## Identifiers

**CAS registry numbers**

- 2821793-99-9

**ChEMBL ID**

CHEMBL6068173

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068173)

**InChIKey**

XXWMEQMGQNHRAF-WFJRNIGCSA-N

Source: [gsrs.ncats.nih.gov](https://gsrs.ncats.nih.gov/ginas/app/beta/substances/3NQ4ME292X)

**PubChem compound IDs**

- 164875418

**FDA ingredient codes (UNII)**

- 3NQ4ME292X

## Regulatory information

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

## Pharmacology

### Drug classification

**Drug name stem**

\-rasib

### Investigated indications

- **Condition**  
Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000616

**Subject identifier**  
D009369

### Open Targets indications (6)

- **Condition identifier**  
EFO\_0000616
- **Condition identifier**  
MONDO\_0005070
- **Condition identifier**  
MONDO\_0005184

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005233

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0006047

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0009831

**Highest recorded phase**  
3

## Chemical properties

**Calculated partition coefficient (XLogP)**

7.7

**Prodrug**

No

**Chirality**

Single enantiomer

**Inorganic**

No

**Heavy atoms**

81

**Monoisotopic mass**

1116.48039179

**Natural product**

No

## Related records

### Trials (4)

- [A Study of ASP3082 in Adults With Advanced Solid Tumors](https://trialight.com/data/trial/a-study-of-asp3082-in-adults-with-advanced-solid-tumors-59ee7502-0056-4353-8442-cb774f9d25f5.md)
- A Study to Compare Setidegrasib (ASP3082) With Docetaxel, in People With Non-small Cell Lung Cancer With a KRAS G12D Mutation
- A Study to Evaluate the Effectiveness and Safety of Setidegrasib, Given With Either mFOLFIRINOX or NALIRIFOX Chemotherapies, in People With Pancreatic Cancer
- A Study to Learn How Fluconazole, Carbamazepine and Itraconazole Affect How the Body Processes ASP3082 in Healthy Adults

### In development for (1)

- Neoplasm Phase 2

---

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