> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/casdatifan-bbad1c6e-e20a-41c3-a739-d7f295439886
> Record changed: 2026-10-13

# Casdatifan

Highest phase reached

Phase 2

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068220)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068220)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 2

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068220)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068220)

**Drug name**

Casdatifan

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068220)

**Structure (SMILES)**

c1cc(c2c(c1S(C)(=O)=O)\[C@@H\](\[C@@H\](C2)F)O)\[C@@\]3(c4c(cc(F)cc4C#N)\[C@H\](\[C@H\](C3)F)F)\[H\]

Source: [gsrs.ncats.nih.gov](https://gsrs.ncats.nih.gov/ginas/app/beta/substances/DP73UWL6LE)

### Other names (12)

- ab 521
- AB-521
- ab521
- AB521
- casdatifan
- Casdatifan
- casdatifan \[INN\]
- CASDATIFAN \[USAN\]
- Casdatifan \[WHO-DD\]
- casdatifan inn
- casdatifan usan
- casdatifan who dd

## Identifiers

**CAS registry numbers**

- 2709069-30-5

**ChEMBL ID**

CHEMBL6068220

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068220)

**InChIKey**

KHBHHNNBNHHGPE-QCCZFBHPSA-N

Source: [gsrs.ncats.nih.gov](https://gsrs.ncats.nih.gov/ginas/app/beta/substances/DP73UWL6LE)

**PubChem compound IDs**

- 156859185

**FDA ingredient codes (UNII)**

- DP73UWL6LE

## Regulatory information

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

## Pharmacology

### Drug classification

**Pharmacology name**

casdatifan

**Type**

Synthetic organic

**Drug name stem**

\-ifan

### Mechanisms of action

- **Action**  
Binding

**Action type**  
Binding

**Target**  
endothelial PAS domain protein 1

**Gene symbol**  
EPAS1

**Protein identifier**  
Q99814

**Median affinity**

7.54

**Affinity units**  
pIC50

### Investigated indications

- **Condition**  
Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000616

**Subject identifier**  
D009369

### Open Targets indications (3)

- **Condition identifier**  
EFO\_0000616
- **Condition identifier**  
MONDO\_0005005

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0005070

## Chemical properties

**Calculated partition coefficient (XLogP)**

3

**Prodrug**

No

**Chirality**

Single enantiomer

**Inorganic**

No

**Heavy atoms**

30

**Monoisotopic mass**

439.08652723

**Natural product**

No

## Related records

### Trials (12)

- A Bioequivalence Study Between Two Casdatifan Tablet Strengths and Food Effect Study of Casdatifan in Healthy Adult Participants
- [A Phase 1 Study of AB521 Monotherapy and Combination Therapies in Renal Cell Carcinoma and Other Solid Tumors](https://trialight.com/data/trial/a-phase-1-study-of-ab521-monotherapy-and-combination-e1b2f8d0-943b-4fb4-a208-30e7ab9efff0.md)
- A Relative Bioavailability Study and Food Effect Study of AB521 in Healthy Adult Volunteers
- [A Study to Evaluate the Safety, Tolerability, and Efficacy of Pumitamig Alone or in Combination With Other Agents in Participants With Advanced Renal Cell Carcinoma (RCC) (ROSETTA RCC-208)](https://trialight.com/data/trial/a-study-to-evaluate-the-safety-tolerability-and-efficacy-of-f09db6b0-53bf-442e-9885-43e7225ef84f.md)
- A Study to Investigate the Efficacy and Safety of Volrustomig ± Casdatifan vs Nivolumab + Ipilimumab as 1L Treatment for Advanced ccRCC
- Comparative PK Assessment Study of Casdatifan in Moderate Hepatically Impaired Participants Versus Matched Participants With Normal Hepatic Function
- Drug-Drug Interaction Study of Casdatifan in Healthy Adult Participants (ARC-29)
- Pilot Study of Casdatifan-Treated Refractory Renal Cell Carcinoma
- Pre-NEOSHIFT-RCC: Neoadjuvant HIF-Inhibitor Immunotherapy in RCC
- Study of Casdatifan and Cabozantinib Versus Placebo and Cabozantinib in Patients With Advanced Clear Cell Renal Cell Carcinoma
- Study of Zanzalintinib (XL092) + AB521 and Zanzalintinib + AB521 + Nivolumab in Participants With Advanced Clear Cell Renal Cell Carcinoma (ccRCC) or Other Advanced Solid Tumors (STELLAR-009)
- Study to Investigate the Safety, Tolerability, and Pharmacokinetic Profile With Oral AB521 in Healthy Volunteers

### In development for (1)

- Neoplasm Phase 2

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