General Information of This Drug (ID: DMT4QHD)

Drug Name
GDC-0032   DMT4QHD
Synonyms
Taselisib; 1282512-48-4; GDC 0032; UNII-L08J2O299M; 2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide; CHEMBL2387080; GDC0032; L08J2O299M; Taselisib [INN]; 2-Methyl-2-(4-{2-[3-Methyl-1-(Propan-2-Yl)-1h-1,2,4-Triazol-5-Yl]-5,6-Dihydroimidazo[1,2-D][1,4]benzoxazepin-9-Yl}-1h-Pyrazol-1-Yl)propanamide; Taselisib [USAN:INN]; GTPL7794; SCHEMBL1485247; SYN1202; DTXSID00155842; BEUQXVWXFDOSAQ-UHFFFAOYSA-N
Indication
Disease Entry ICD 11 Status REF
Breast cancer 2C60-2C65 Phase 3 [1]
Solid tumour/cancer 2A00-2F9Z Phase 2/3 [2]
Drug Type
Small molecular drug
Structure
3D MOL is unavailable 2D MOL

List of Combinatorial Drugs (CBD) Containing This Drug

4 Investigative Drug Combination(s) Consisting of This drug
Normalized Drug Combination Synergy Score
Synergy scores were normalized using Min-Max Scaling to facilitate visual comparisons.
DrugCom Name DrugCom ID Component Drug Indication REF
GDC-0032 + Lumefantrine DCRF4WC Lumefantrine DD2 (Cell Line: DD2) [3]
GDC-0032 + Marizomib DC6E335 Marizomib Diffuse intrinsic pontine glioma (Cell Line: DIPG25) [3]
GDC-0032 + Lumefantrine DCC7934 Lumefantrine Hepatoblastoma (Cell Line: HB3) [4]
Lumefantrine + GDC-0032 DC8DKRV Lumefantrine DD2 (Cell Line: DD2) [3]
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5 Clinical Trial Drug Combination(s) Consisting of This drug
DrugCom Name DrugCom ID Component Drug Indication REF
Docetaxel + GDC-0032 DCJFMX0 Docetaxel Breast Cancer, Non-small Lung Cancer [5]
Enzalutamide + GDC-0032 DCAIW4U Enzalutamide Estrogen Receptor Negative [6]
Fulvestrant + GDC-0032 DCKZ7CR Fulvestrant Solid Cancers [7]
GDC-0032 + Midazolam DC1RFA1 Midazolam Solid Cancers [7]
Letrozole + GDC-0032 DCLZ8LP Letrozole Solid Cancers [7]
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References

1 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7794).
3 Recurrent recessive mutation in deoxyguanosine kinase causes idiopathic noncirrhotic portal hypertension.Hepatology. 2016 Jun;63(6):1977-86. doi: 10.1002/hep.28499. Epub 2016 Mar 31.
4 Loss of function mutations in VARS encoding cytoplasmic valyl-tRNA synthetase cause microcephaly, seizures, and progressive cerebral atrophy.Hum Genet. 2018 Apr;137(4):293-303. doi: 10.1007/s00439-018-1882-3. Epub 2018 Apr 24.
5 ClinicalTrials.gov (NCT01862081) A Dose-escalation Study to Assess the Safety, Tolerability, and Pharmacokinetics of GDC-0032 in Combination With Docetaxel or With Paclitaxel in Patients With HER2-negative Locally Recurrent or Metastatic Breast Cancer or Non-small Cell Lung Cancer
6 ClinicalTrials.gov (NCT02457910) Taselisib and Enzalutamide in Treating Patients With Androgen Receptor Positive Triple-Negative Metastatic Breast Cancer
7 ClinicalTrials.gov (NCT01296555) A Dose Escalation Study Evaluating the Safety and Tolerability of GDC-0032 in Participants With Locally Advanced or Metastatic Solid Tumors or Non-Hodgkin's Lymphoma (NHL) and in Combination With Endocrine Therapy in Locally Advanced or Metastatic Hormone Receptor-Positive Breast Cancer