Dactolisib
Highest phase reached
Phase 3
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Phase 3
- Drug type
- Small molecule
- Drug name
- Dactolisib
- Molecular weight
- 469.55
- Structure (SMILES)
- Cn1c(=O)n(-c2ccc(C(C)(C)C#N)cc2)c2c3cc(-c4cnc5ccccc5c4)ccc3ncc21
- 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.
- CAS registry numbers
- 915019-65-7
- ChEMBL ID
- CHEMBL1879463
- InChIKey
- JOGKUKXHTYWRGZ-UHFFFAOYSA-N
- PubChem compound IDs
- 11977753
- FDA ingredient codes (UNII)
- RUJ6Z9Y0DT
- First in class
- No
- Orphan designation
- No
- Pharmacology name
- dactolisib
- Type
- Synthetic organic
- Drug name stem
- -lisib
- 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
- 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
- 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
- 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.
- 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
- NCT01195376
- NCT01337765
- NCT01343498
- NCT01690871
- NCT01248494
- NCT01288092
- NCT01495247
- NCT01290406
- NCT01453595
- NCT01508104
- NCT01628913
- NCT01658436
- NCT01634061
- NCT01717898
- NCT01856101
- NCT03373903
- NCT04668352
- NCT04409327
- NCT04584710
- 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
- Recorded assays
- 2,183
- Active assays
- 1,373
- Confirmatory
- Other
- Screening
- Antineoplastic Agents
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)
- 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
- 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 Phase 2
- Cancer Phase 2
- COVID-19 Phase 2
- Endometrial cancer Phase 2
- Kidney cancer Phase 1
- Neoplasm Phase 2
- Pancreatic neuroendocrine tumor Phase 2
- Prostate cancer Phase 1
- Transitional cell carcinoma Phase 2
Targets (9)
- MTOR Serine/threonine-protein kinase mTOR inhibitor
- PIK3CA PI3-kinase class I inhibitor
- PIK3CB PI3-kinase class I inhibitor
- PIK3CD PI3-kinase class I inhibitor
- PIK3CG PI3-kinase class I inhibitor
- PIK3R1 PI3-kinase class I inhibitor
- PIK3R2 PI3-kinase class I inhibitor
- PIK3R3 PI3-kinase class I inhibitor
- PIK3R5 PI3-kinase class I inhibitor