> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/gedatolisib-ab488a0b-b1b9-4660-9c36-3e706274ef7a
> Record changed: 2026-10-13

# Gedatolisib

Highest phase reached

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL592445)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL592445)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL592445)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL592445)

**Drug name**

Gedatolisib

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL592445)

**Molecular weight**

615.74

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL592445)

**Structure (SMILES)**

CN(C)C1CCN(C(=O)c2ccc(NC(=O)Nc3ccc(-c4nc(N5CCOCC5)nc(N5CCOCC5)n4)cc3)cc2)CC1

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL592445)

### Other names (16)

- gedatolisib
- Gedatolisib
- gedatolisib \[INN\]
- GEDATOLISIB \[USAN\]
- Gedatolisib \[WHO-DD\]
- gedatolisib inn
- gedatolisib usan
- gedatolisib who dd
- pf 05212384
- PF-05212384
- PF-05212384 (also known as PKI-587)
- PF-05212384 (gedatolisib)
- pki 587
- PKI-587
- revtorpyk
- REVTORPYK

## Identifiers

**CAS registry numbers**

- 1197160-78-3

**ChEMBL ID**

CHEMBL592445

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL592445)

**InChIKey**

DWZAEMINVBZMHQ-UHFFFAOYSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL592445)

**PubChem compound IDs**

- 44516953

**FDA ingredient codes (UNII)**

- 96265TNH2R

## Regulatory information

### Other regulatory facts

**Patents**

0

**Designations**

1

**First in class**

No

**Fast track**

No

**Breakthrough designation**

Yes

**Orphan designation**

No

**Priority review**

No

**Orphan exclusivity**

No

**Accelerated approval**

No

## Pharmacology

### Drug classification

**Pharmacology name**

gedatolisib

**Type**

Synthetic organic

**Drug name stem**

\-lisib

### Mechanisms of action (11)

- **Action**  
Inhibition

**Action type**  
Inhibitor

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

**Gene symbol**  
PIK3CA

**Protein identifier**  
P42336

**Median affinity**

9.4

**Affinity units**  
pIC50

**Primary target**  
Yes
- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
mechanistic target of rapamycin kinase

**Gene symbol**  
MTOR

**Protein identifier**  
P42345

**Median affinity**

8.8

**Affinity units**  
pIC50

**Primary target**  
Yes
- **Mechanism**  
PI3-kinase class I inhibitor

**Action type**  
Inhibitor

**Target**  
PI3-kinase class I

**Protein identifier**  
O00329
- **Mechanism**  
PI3-kinase class I inhibitor

**Action type**  
Inhibitor

**Target**  
PI3-kinase class I

**Protein identifier**  
O00459
- **Mechanism**  
PI3-kinase class I inhibitor

**Action type**  
Inhibitor

**Target**  
PI3-kinase class I

**Protein identifier**  
P27986
- **Mechanism**  
PI3-kinase class I inhibitor

**Action type**  
Inhibitor

**Target**  
PI3-kinase class I

**Protein identifier**  
P42336
- **Mechanism**  
PI3-kinase class I inhibitor

**Action type**  
Inhibitor

**Target**  
PI3-kinase class I

**Protein identifier**  
P42338
- **Mechanism**  
PI3-kinase class I inhibitor

**Action type**  
Inhibitor

**Target**  
PI3-kinase class I

**Protein identifier**  
P48736
- **Mechanism**  
PI3-kinase class I inhibitor

**Action type**  
Inhibitor

**Target**  
PI3-kinase class I

**Protein identifier**  
Q8WYR1
- **Mechanism**  
PI3-kinase class I inhibitor

**Action type**  
Inhibitor

**Target**  
PI3-kinase class I

**Protein identifier**  
Q92569
- **Mechanism**  
Serine/threonine-protein kinase mTOR inhibitor

**Action type**  
Inhibitor

**Target**  
Serine/threonine-protein kinase mTOR

**Protein identifier**  
P42345

### Open Targets mechanisms (2)

- **Mechanism**  
PI3-kinase class I inhibitor

**Action type**  
Inhibitor

**Target**  
PI3-kinase class I
- **Mechanism**  
Serine/threonine-protein kinase mTOR inhibitor

**Action type**  
Inhibitor

**Target**  
Serine/threonine-protein kinase mTOR

### Investigated indications (7)

- **Condition**  
Myelodysplastic Syndromes

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000198

**Subject identifier**  
D009190
- **Condition**  
Leukemia, Myeloid, Acute

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000222

**Subject identifier**  
D015470
- **Condition**  
Neoplasms

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0000616

**Subject identifier**  
D009369
- **Condition**  
Carcinoma, Non-Small-Cell Lung

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0003060

**Subject identifier**  
D002289
- **Condition**  
Endometrial Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0004230

**Subject identifier**  
D016889
- **Condition**  
Neoplasms

**Highest recorded phase**  
1

**Condition identifier**  
MONDO:0004992

**Subject identifier**  
D009369
- **Condition**  
Breast Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
MONDO:0007254

**Subject identifier**  
D001943

### Open Targets indications (26)

- **Condition identifier**  
EFO\_0000198

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000222

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000616

**Highest recorded phase**  
1
- **Condition identifier**  
EFO\_0003060
- **Condition identifier**  
EFO\_0004230

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0002447

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

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005070

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005097

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005170

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005192

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005206

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005233

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005494

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005575

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005627

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

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0008170

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0008315

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0008433

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0009831

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0011962

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0018177

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0018874

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0018881

**Highest recorded phase**  
2

And 1 more, listed on the interactive page.

### Reported adverse events (2)

- **Event**  
escherichia bacteraemia

**Reports**  
5

**Reporting signal score**

31.1533
- **Event**  
hyperglycaemia

**Reports**  
5

**Reporting signal score**

17.1313

### Trial references (12)

- NCT00940498  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00940498)
- NCT01920061  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01920061)
- NCT01347866  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01347866)
- NCT01420081  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01420081)
- NCT02438761  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02438761)
- NCT02626507  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02626507)
- NCT02684032  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02684032)
- NCT03243331  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03243331)
- NCT03400254  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03400254)
- NCT03698383  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03698383)
- NCT05501886  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05501886)
- NCT02920450  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02920450)

## Chemical properties

**Hydrogen bond acceptors**

10

**Hydrogen bond donors**

2

**Polar surface area**

128.29

**Calculated partition coefficient (ALogP)**

3.02

**Calculated partition coefficient (XLogP)**

2.4

**Prodrug**

No

**Chirality**

Achiral

**Inorganic**

No

**Rule-of-five violations**

1

**Rotatable bonds**

7

**Heavy atoms**

45

**Molecular formula**

C32H41N9O4

**Monoisotopic mass**

615.32815082

**Natural product**

Yes

## Evidence counts

**Recorded assays**

941

**Active assays**

375

### Active assay types (3)

- Confirmatory
- Other
- Screening

## Pharmacologic actions

- Protein Kinase Inhibitors  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D047428.html)

## Biological measurements

### Observed measurements

#### Solubility

**Median**

14.5

**Mean**

14.5

**Minimum**

14

**Maximum**

15

**Unit**

ug/mL

**Assays**

2

**Standard deviation**

0.707107

**Summary method**

median

**Censored results excluded**

0

**Other units excluded**

0

**Unknown units excluded**

0

#### Measurement types

- Solubility

## Related records

### Trials (22)

- A Study Of PF-05212384 In Combination With Other Anti-Tumor Agents and in Combination With Cisplatin in Patients With Triple Negative Breast Cancer in an Expansion Arm (TNBC)
- A Study Of PF-05212384 Plus FOLFIRI Versus Bevacizumab Plus FOLFIRI In Metastatic Colorectal Cancer
- A Study Of PF-05212384 Plus Irinotecan Vs Cetuximab Plus Irinotecan In Patients With KRAS And NRAS Wild Type Metastatic Colorectal Cancer
- A Study Of Two Dual PI3K/mTOR Inhibitors, PF-04691502 And PF-05212384 In Patients With Recurrent Endometrial Cancer
- A Study To Assess The Tolerability And Clinical Activity Of Gedatolisib In Combination With Palbociclib/Letrozole Or Palbociclib/Fulvestrant In Women With Metastatic Breast Cancer
- An Initial Safety Study of Gedatolisib Plus PTK7-ADC for Metastatic Triple-negative Breast Cancer
- Clinical Study Of PI3K/mTOR Inhibitors In Combination With An Oral MEK Inhibitor Or Irinotecan In Patients With Advanced Cancer
- Dose Finding Study Of PF-05212384 With Paclitaxel And Carboplatin In Patients With Advanced Solid Tumor
- Expanded Access Protocol for Subjects Previously Treated With Gedatolisib in B2151009
- Gedatolisib in Combination With Darolutamide in Metastatic Castration-Resistant Prostate Cancer
- Gedatolisib Plus Fulvestrant With or Without Palbociclib vs Standard-of-Care for the Treatment of Patients With Advanced or Metastatic HR+/HER2- Breast Cancer (VIKTORIA-1)
- Gedatolisib Plus Talazoparib in Advanced Triple Negative or BRCA1/2 Positive, HER2 Negative Breast Cancers
- Gedatolisib, Hydroxychloroquine or the Combination for Prevention of Recurrent Breast Cancer ("GLACIER")
- Investigation Of The Metabolism, And Excretion Of \[14c\]-PF-05212384 In Healthy Male Volunteers
- PF-05212384 (PKI-587) for t-AML/MDS or de Novo Relapsed or Refractory Acute Myeloid Leukemia (AML) (LAM-PIK)
- [Phase 3 Study of Gedatolisib as First-Line Treatment for Patients With HR-Positive, HER2-Negative Advanced Breast Cancer (VIKTORIA-2)](https://trialight.com/data/trial/phase-3-study-of-gedatolisib-as-first-line-treatment-for-b45309b2-db0c-489d-a3ba-d60f535b62ba.md)
- Phase I Study of Combination of Gedatolisib With Palbociclib and Faslodex in Patients With ER+/HER2- Breast Cancer
- Phase II Study of Herzuma® Plus Gedatolisib in Patients With HER-2 Positive Metastatic Breast Cancer
- RESOLVE: Abemaciclib + Letrozole +/- Metformin or Gedatolisib in Endometrial Cancer
- Study of Paclitaxel, Carboplatin, and PF-05212384 in Advanced or Metastatic NSCLC (UF-STO-LUNG-002)

### In development for (7)

- [Acute myeloid leukemia](https://trialight.com/data/condition/acute-myeloid-leukemia-b0971a7a-c18d-544e-bd7f-b1a13b9caa30.md) Phase 2
- [Breast cancer](https://trialight.com/data/condition/breast-cancer-8ac10da3-93bd-54c5-a93b-265bc6699689.md) Phase 3
- [Cancer](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md) Phase 1
- [Endometrial carcinoma](https://trialight.com/data/condition/endometrial-carcinoma-d0794a04-ff16-5af6-8fb7-7b3d6bd6c537.md) Phase 2
- [Myelodysplastic syndrome](https://trialight.com/data/condition/myelodysplastic-syndrome-f5df8ce5-6064-53d3-902c-f09fc4acd4bb.md) Phase 2
- Neoplasm Phase 1
- [Non-small cell lung carcinoma](https://trialight.com/data/condition/non-small-cell-lung-carcinoma-a86c1d60-523f-5ea7-a5e1-39ed4a2296f8.md) Phase 1

### Targets (9)

- [MTOR](https://trialight.com/data/target/mtor-b7a8666b-fb4c-536c-9a22-e9676e041efb.md) Serine/threonine-protein kinase mTOR inhibitor
- [PIK3CA](https://trialight.com/data/target/pik3ca-02cdda4d-e060-5df2-a713-4b081b6bb7bc.md) PI3-kinase class I inhibitor
- [PIK3CB](https://trialight.com/data/target/pik3cb-97c45181-3c9e-530e-8a15-5b652b9b6958.md) PI3-kinase class I inhibitor
- [PIK3CD](https://trialight.com/data/target/pik3cd-aa1d8478-0790-59e6-92da-df04eb62d806.md) PI3-kinase class I inhibitor
- [PIK3CG](https://trialight.com/data/target/pik3cg-cf34f1e3-ab4a-550a-9e84-6fb39401d9c1.md) PI3-kinase class I inhibitor
- [PIK3R1](https://trialight.com/data/target/pik3r1-75490e88-a83a-5c97-9c49-82b67f3d873f.md) PI3-kinase class I inhibitor
- [PIK3R2](https://trialight.com/data/target/pik3r2-c5a9439c-0e76-5ccf-b39e-f3c8a19e8bfc.md) PI3-kinase class I inhibitor
- [PIK3R3](https://trialight.com/data/target/pik3r3-95f9f6b6-7509-5622-a188-d884a2500d0c.md) PI3-kinase class I inhibitor
- [PIK3R5](https://trialight.com/data/target/pik3r5-e2261b65-f6ce-59f8-8444-c6cf72c5cbac.md) PI3-kinase class I inhibitor

---

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