> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/dactolisib-c690af54-bc20-4e80-bd3c-2db9669c43d1
> Record changed: 2026-10-13

# Dactolisib

Highest phase reached

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1879463)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1879463)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1879463)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1879463)

**Drug name**

Dactolisib

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1879463)

**Molecular weight**

469.55

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1879463)

**Structure (SMILES)**

Cn1c(=O)n(-c2ccc(C(C)(C)C#N)cc2)c2c3cc(-c4cnc5ccccc5c4)ccc3ncc21

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1879463)

### Other names (27)

- bez 235
- Bez-235
- BEZ-235
- bez235
- BEZ235
- BEZ235 (Stage 1)
- dactolisib
- Dactolisib
- dactolisib \[INN\]
- DACTOLISIB \[USAN\]
- Dactolisib \[WHO-DD\]
- dactolisib inn
- dactolisib usan
- dactolisib who dd
- nsc 751249
- NSC-751249
- nvp bez 235
- nvp bez235
- nvp bez235 nx
- Nvp-bez-235
- NVP-BEZ235
- NVP-BEZ235-NX
- rtb 101
- RTB-101
- rtb101

And 2 more, listed on the interactive page.

## Identifiers

**CAS registry numbers**

- 915019-65-7

**ChEMBL ID**

CHEMBL1879463

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1879463)

**InChIKey**

JOGKUKXHTYWRGZ-UHFFFAOYSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1879463)

**PubChem compound IDs**

- 11977753

**FDA ingredient codes (UNII)**

- RUJ6Z9Y0DT

## Regulatory information

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

## Pharmacology

### Drug classification

**Pharmacology name**

dactolisib

**Type**

Synthetic organic

**Drug name stem**

\-lisib

### Mechanisms of action (14)

- **Action**  
Inhibition

**Action type**  
Inhibitor

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

**Gene symbol**  
PIK3CD

**Protein identifier**  
O00329

**Median affinity**

8.15

**Affinity units**  
pIC50

**Primary target**  
Yes
- **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

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

**Action type**  
Inhibitor

**Target**  
mechanistic target of rapamycin kinase

**Gene symbol**  
MTOR

**Protein identifier**  
P42345

**Median affinity**

8.22

**Affinity units**  
pIC50

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

**Action type**  
Inhibitor

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

**Gene symbol**  
PIK3CG

**Protein identifier**  
P48736

**Median affinity**

8.3

**Affinity units**  
pIC50

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

**Action type**  
Inhibitor

**Target**  
ATR checkpoint kinase

**Gene symbol**  
ATR

**Protein identifier**  
Q13535

**Median affinity**

7.68

**Affinity units**  
pIC50
- **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 (10)

- **Condition**  
Infections

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000544

**Subject identifier**  
D007239
- **Condition**  
Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000616

**Subject identifier**  
D009369
- **Condition**  
Neuroendocrine Tumors

**Highest recorded phase**  
2

**Condition identifier**  
EFO:1000045

**Subject identifier**  
D018358
- **Condition**  
Carcinoma, Transitional Cell

**Highest recorded phase**  
2

**Condition identifier**  
EFO:1000601

**Subject identifier**  
D002295
- **Condition**  
Kidney Neoplasms

**Highest recorded phase**  
1

**Condition identifier**  
MONDO:0002367

**Subject identifier**  
D007680
- **Condition**  
Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0004992

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

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0007254

**Subject identifier**  
D001943
- **Condition**  
Prostatic Neoplasms, Castration-Resistant

**Highest recorded phase**  
1

**Condition identifier**  
MONDO:0008315

**Subject identifier**  
D064129
- **Condition**  
Endometrial Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0011962

**Subject identifier**  
D016889
- **Condition**  
Severe Acute Respiratory Syndrome

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0100096

**Subject identifier**  
D045169

### Open Targets indications (26)

- **Condition identifier**  
EFO\_0000544

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0000616

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_1000045

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_1000601

**Highest recorded phase**  
2
- **Condition identifier**  
HP\_0011947

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0002367
- **Condition identifier**  
MONDO\_0002367

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0002447

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0004967

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0004992

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005070

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005086

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005105

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

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

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005549

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

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0006115

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0006474

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0007254

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0008315

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

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

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0018874

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0019954

**Highest recorded phase**  
2

And 1 more, listed on the interactive page.

### Reported adverse events (8)

- **Event**  
anal inflammation

**Reports**  
1

**Reporting signal score**

6.62964
- **Event**  
clonal evolution

**Reports**  
3

**Reporting signal score**

26.3815
- **Event**  
dysgeusia

**Reports**  
2

**Reporting signal score**

5.60335
- **Event**  
ectopic hormone secretion

**Reports**  
3

**Reporting signal score**

34.6518
- **Event**  
hypercalcaemia

**Reports**  
3

**Reporting signal score**

13.0245
- **Event**  
neurilemmoma malignant

**Reports**  
1

**Reporting signal score**

9.97322
- **Event**  
pneumonitis

**Reports**  
2

**Reporting signal score**

6.66674
- **Event**  
weight decreased

**Reports**  
3

**Reporting signal score**

5.98605

### Trial references (19)

- NCT01195376  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01195376)
- NCT01337765  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01337765)
- NCT01343498  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01343498)
- NCT01690871  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01690871)
- NCT01248494  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01248494)
- NCT01288092  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01288092)
- NCT01495247  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01495247)
- NCT01290406  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01290406)
- NCT01453595  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01453595)
- NCT01508104  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01508104)
- NCT01628913  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01628913)
- NCT01658436  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01658436)
- NCT01634061  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01634061)
- NCT01717898  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01717898)
- NCT01856101  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01856101)
- NCT03373903  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03373903)
- NCT04668352  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04668352)
- NCT04409327  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04409327)
- NCT04584710  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04584710)

## Chemical properties

**Hydrogen bond acceptors**

6

**Hydrogen bond donors**

0

**Polar surface area**

76.5

**Calculated partition coefficient (ALogP)**

5.89

**Calculated partition coefficient (XLogP)**

5.2

**Prodrug**

No

**Chirality**

Achiral

**Inorganic**

No

**Rule-of-five violations**

1

**Rotatable bonds**

3

**Heavy atoms**

36

**Molecular formula**

C30H23N5O

**Monoisotopic mass**

469.19026037

**Natural product**

Yes

## Evidence counts

**Recorded assays**

2,183

**Active assays**

1,373

### Active assay types (3)

- Confirmatory
- Other
- Screening

## Pharmacologic actions

- Antineoplastic Agents  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000970.html)

## Biological measurements

### Observed measurements

#### Distribution coefficient (LogD)

**Median**

6.44

**Mean**

6.44

**Minimum**

6.44

**Maximum**

6.44

**Unit**

unitless

**Assays**

1

**Standard deviation**

0

**Summary method**

median

**Censored results excluded**

0

**Other units excluded**

0

**Unknown units excluded**

0

#### Measurement types

- LogD

#### Solubility

**Median**

19,000

**Mean**

19,000

**Minimum**

19,000

**Maximum**

19,000

**Unit**

nM

**Assays**

1

**Standard deviation**

0

**Summary method**

median

**Censored results excluded**

0

**Other units excluded**

0

**Unknown units excluded**

0

#### Measurement types

- Solubility

#### Oral bioavailability

**Median**

37.82

**Mean**

37.82

**Minimum**

37.82

**Maximum**

37.82

**Unit**

%

**Assays**

1

**Standard deviation**

0

**Summary method**

median

**Censored results excluded**

0

**Other units excluded**

0

**Unknown units excluded**

0

#### Measurement types

- F

## Related records

### Trials (34)

- [A Clinical Study of Novel Pneumococcal Vaccine V118C in Children (V118C-002)](https://trialight.com/data/trial/a-clinical-study-of-novel-pneumococcal-vaccine-v118c-in-d6487b9b-a525-4860-bc13-9338ed58336d.md)
- A Multicenter Phase I/II Trial of Abiraterone Acetate + BEZ235 in Metastatic, Castration-Resistant Prostate Cancer
- A Pharmacokinetics Study to Assess Abiraterone Acetate Capsule and Tablet Formulations in Patients With Prostate Cancer
- A Phase 2 Study of RTB101 as COVID-19 Post-Exposure Prophylaxis in Older Adults
- A Phase I, Dose-finding Study of BEZ235 in Adult Patients With Relapsed or Refractory Acute Leukemia
- A Phase I/II Study of BEZ235 in Patients With Advanced Solid Malignancies Enriched by Patients With Advanced Breast Cancer
- [A Phase Ib Study of HS-10352 Plus Fulvestrant in Patients With Advanced Breast Cancer](https://trialight.com/data/trial/a-phase-ib-study-of-hs-10352-plus-fulvestrant-in-patients-605bb4d0-2890-4f1e-baa7-099019096c00.md)
- A Phase Ib/II Study of BEZ235 and Trastuzumab in Patients With HER2-positive Breast Cancer Who Failed Prior to Trastuzumab
- A Phase II Study of Orally Administered BEZ235 Monotherapy in Patients With Metastatic or Unresectable Malignant PEComa
- A Study of BEZ235 in Adult Japanese Patients With Advanced Solid Tumors
- A Study of GSK2110183 in Subjects With Proteasome Inhibitor Refractory Multiple Myeloma
- A Trial of Oral BEZ235 and BKM120 in Combination With Paclitaxel With or Without Trastuzumab
- BEZ235 in Patients With Advanced Renal Cell Carcinoma (RCC)
- BEZ235 Phase II Trial in Patients With Advanced Pancreatic Neuroendocrine Tumors (pNET) After Failure of mTOR Inhibitor Therapy.
- BEZ235 Trial in Patients With Advanced Endometrial Carcinoma
- BEZ235 Trial in Patients With HER2-(Human Epidermal Growth Factor Receptor 2 Negative) /HR+ (Hormonal Receptor Positive) Metastatic Breast Cancer
- Dose Finding Study of RAD001 (Everolimus, Afinitor®) in Combination With BEZ235 in Patients With Advanced Solid Tumors
- Dose Finding Study to Determine if BEZ235 Alone or in Combination With RAD001 Decreases the Incidence of Respiratory Tract Infections in the Elderly
- Efficacy and Safety of BEZ235 Compared to Everolimus in Patients With Advanced Pancreatic Neuroendocrine Tumors
- Efficacy and Safety of GNR-038 vs Berinert® in Patients With Hereditary Angioedema

### In development for (9)

- [Breast cancer](https://trialight.com/data/condition/breast-cancer-8ac10da3-93bd-54c5-a93b-265bc6699689.md) Phase 2
- [Cancer](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md) Phase 2
- [COVID-19](https://trialight.com/data/condition/covid-19-13f0ebf3-c291-557d-bdef-93563d077103.md) Phase 2
- [Endometrial cancer](https://trialight.com/data/condition/endometrial-cancer-4da2a0bc-7943-502b-a698-cc2beccbed8c.md) Phase 2
- Kidney cancer Phase 1
- Neoplasm Phase 2
- Pancreatic neuroendocrine tumor Phase 2
- [Prostate cancer](https://trialight.com/data/condition/prostate-cancer-3659fc70-617b-5868-a093-ae819ffc6755.md) Phase 1
- [Transitional cell carcinoma](https://trialight.com/data/condition/transitional-cell-carcinoma-19611feb-3997-59b1-ad3d-49b845cbe40f.md) Phase 2

### 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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