> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/rly-2608-73ce28bc-f8a2-48ce-83f9-acf75bdfd6ac
> Record changed: 2026-10-13

# RLY-2608

Highest phase reached

Phase 1

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068523)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068523)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 1

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068523)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068523)

**Drug name**

RLY-2608

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068523)

**Molecular weight**

608.91

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068523)

**Structure (SMILES)**

N#Cc1c(-c2cc(NC(=O)c3cc(F)cc(C(F)(F)F)c3)c3c(c2)C(=O)N\[C@H\]3c2cc(F)ccc2Cl)ccc2ncnn12

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068523)

### Other names (21)

- acc 602
- ACC-602
- c200825002 fp
- C200825002-FP
- rly 2608
- RLY 2608
- Rly-2608
- RLY-2608
- rly2608
- RLY2608
- rtx 1274076
- rtx 4076
- RTX-1274076
- RTX-4076
- zovegalisib
- Zovegalisib
- ZOVEGALISIB
- zovegalisib \[INN\]
- ZOVEGALISIB \[USAN\]
- zovegalisib inn
- zovegalisib usan

## Identifiers

**CAS registry numbers**

- 2733573-94-7

**ChEMBL ID**

CHEMBL6068523

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068523)

**InChIKey**

VYWRYBZVVSPTQN-SANMLTNESA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL6068523)

**PubChem compound IDs**

- 166822065

**FDA ingredient codes (UNII)**

- LR5XLA3BPC

## Regulatory information

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

## Pharmacology

### Drug classification

**Pharmacology name**

zovegalisib

**Type**

Synthetic organic

### Mechanisms of action (3)

- **Action type**  
Inhibitor

**Target**  
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha

**Gene symbol**  
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha

**Gene symbol**  
PIK3CA

**Protein identifier**  
P42336

**Median affinity**

7.32

**Affinity units**  
pIC50
- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha

**Gene symbol**  
PIK3CA

**Protein identifier**  
P42336

**Median affinity**

8.4

**Affinity units**  
pIC50

### Open Targets indications (4)

- **Condition identifier**  
EFO\_0009146

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0004992

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0007254

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_1040002

**Highest recorded phase**  
2

## Chemical properties

**Hydrogen bond acceptors**

6

**Hydrogen bond donors**

2

**Polar surface area**

112.18

**Calculated partition coefficient (ALogP)**

6.3

**Calculated partition coefficient (XLogP)**

5.5

**Prodrug**

No

**Chirality**

Single enantiomer

**Inorganic**

No

**Rule-of-five violations**

2

**Rotatable bonds**

4

**Heavy atoms**

43

**Molecular formula**

C29H14ClF5N6O2

**Monoisotopic mass**

608.0786922

**Natural product**

No

## Evidence counts

**Recorded assays**

59

**Active assays**

4

### Active assay types

- Confirmatory

## Related records

### Trials (3)

- [A Phase 2 Study of Mutant-selective PI3Kα Inhibitor, RLY-2608, in Adults and Children With PIK3CA Related Overgrowth Spectrum and Malformations Driven by PIK3CA Mutation (The ReInspire Study)](https://trialight.com/data/trial/a-phase-2-study-of-mutant-selective-pi3k-inhibitor-rly-2608-cb48d7d4-b39e-48fc-b89b-e54745cb8b7c.md)
- [First-in-Human Study of Mutant-selective PI3Kα Inhibitor, RLY-2608, as a Single Agent in Patients With Advanced Solid Tumors and in Combination With Endocrine Therapy +/- a CDK4/6 or CDK4 Inhibitor in Patients With Advanced Solid Tumors or Advanced Breast Cancer](https://trialight.com/data/trial/first-in-human-study-of-mutant-selective-pi3k-inhibitor-rly-9e76b9f6-c935-4570-b239-0dc9755a4b4e.md)
- Phase 3 Study of RLY-2608 + Fulvestrant vs Capivasertib + Fulvestrant as Treatment for Locally Advanced or Metastatic PIK3CA-mutant HR+/HER2- Breast Cancer

---

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