taselisib
Small moleculeexperimental
Taselisib is a former cancer drug candidate that was in development by Roche. It is a small molecule phosphoinositide 3-kinase inhibitor targeting the PI3K isoform p110α (PIK3CA). — Wikipedia
Clinical trial activity
16 trials · 19 clinical orgs · 0 marketing orgs
Phase 1
10
Phase 2
7
Phase 3
2
Phase 4
0
Earliest trial started Mar 16, 2011 (NCT01296555)
Timeline
Indications
Studied for
- Bile Duct Neoplasms · Phase 2
- Breast Neoplasms · Phase 3
- Colonic Neoplasms · Phase 2
- Colorectal Neoplasms · Phase 2
- Endometrial Neoplasms · Phase 2
- Esophageal Neoplasms · Phase 2
- Glioma · Phase 2
- Healthy Volunteers · Phase 1
- Kidney Neoplasms · Phase 2
- Liver Neoplasms · Phase 2
- Lung Neoplasms · Phase 2/Phase 3
- Lymphoma · Phase 2
- Lymphoma, Non-Hodgkin · Phase 1
- Melanoma · Phase 2
- Multiple Myeloma · Phase 2
- Neoplasm Metastasis · Phase 2
- Neoplasms · Phase 2
- Ovarian Neoplasms · Phase 2
- Pancreatic Neoplasms · Phase 2
- Prostatic Neoplasms · Phase 2
- Proteus Syndrome · Phase 1/Phase 2
- Skin Neoplasms · Phase 2
- Squamous Cell Carcinoma of Head and Neck · Phase 2
- Stomach Neoplasms · Phase 2
- Thyroid Neoplasms · Phase 2
- Urinary Bladder Neoplasms · Phase 2
- Uterine Cervical Neoplasms · Phase 2
- Uterine Neoplasms · Phase 2
Mechanism of action
- PI3-kinase class IINHIBITOR
PI3-kinase class I inhibitor
Developed as an isoform-specific PI3K inhibitor with compound exhibiting high affinity for mutated PI3Ka )doi:10.1158/1538-7445.AM2013-DDT02-01).
- Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1) ↗
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (PIK3CB) ↗
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (PIK3CG) ↗
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PIK3CA) ↗
- Phosphatidylinositol 3-kinase regulatory subunit beta (PIK3R2) ↗
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PIK3CD) ↗
- Phosphoinositide 3-kinase regulatory subunit 5 (PIK3R5) ↗
- Phosphatidylinositol 3-kinase regulatory subunit gamma (PIK3R3) ↗
- PI3-kinase p85-alpha subunit
- PI3-kinase p110-delta subunit
- PI3-kinase p110-alpha subunit
- PI3-kinase p110-gamma subunit
- PI3-kinase p110-beta subunit
- PI3-kinase p85-beta subunit
- PI3-kinase p110-delta/p85-alpha
- PI3-kinase p110-alpha/p85-alpha
- PI3K p110 beta/p85 alpha
- PI3-kinase subunit gamma/Phosphoinositide 3-kinase regulatory subunit 5
- Phosphatidylinositol 3-kinase regulatory subunit beta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform/gamma isoform
- PIK3CG/PIK3R1
- Phosphatidylinositol 3-kinase regulatory subunit gamma
Chemistry & pharmacology
Loading structure…
SMILES
Cc1nc(-c2cn3c(n2)-c2ccc(-c4cnn(C(C)(C)C(N)=O)c4)cc2OCC3)n(C(C)C)n1- Mol. weight
- 460.54 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaTaselisib ↗
- ChEMBLCHEMBL2387080 ↗
Also known as
- 2-(3-(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
- gdc-0032
- gdc-0032
- gdc-0032
- gdc-0032
- rg-7604
- rg-7604
- taselisib
- taselisib
- taselisib
- taselisib
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03290092 | Phase 1/Phase 2 (Phase 2) | Jul 31, 2017 | University of Burgundy |
| NCT04439175 | Phase 2 | Feb 25, 2016 | ECOG-ACRIN Cancer Research Group, National Cancer Institute (NCI) |
| NCT02465060 | Phase 2 | Aug 12, 2015 | ECOG-ACRIN Cancer Research Group, National Cancer Institute (NCI) |
| NCT02457910 | Phase 1/Phase 2 (Phase 2) | Jun 1, 2015 | Conquer Cancer Foundation, Genentech, National Cancer Institute (NCI), Vanderbilt University |
| NCT02340221 | Phase 3 | Apr 8, 2015 | Roche |
| NCT02390427 | Phase 1 | Apr 1, 2015 | Genentech, Harvard University |
| NCT02389842 | Phase 1 | Feb 1, 2015 | Pfizer, Roche, Royal Marsden Hospital NHS Trust, University of London |
| NCT02273973 | Phase 2 | Nov 12, 2014 | Austrian Breast and Colorectal Cancer Group, Genentech, Roche, SOLTI Breast Cancer Research Group, University of Milan |
| NCT02285179 | Phase 1 | Nov 1, 2014 | European Commission, Genentech, Netherlands Cancer Institute, University of Amsterdam, University of Cambridge |
| NCT02154490 | Phase 2/Phase 3 (Phase 3) | Jun 1, 2014 | National Cancer Institute (NCI), Southwest Oncology Group |
| NCT02785913 | Phase 2 | Jun 1, 2014 | National Cancer Institute (NCI), Southwest Oncology Group |
| NCT01980953 | Phase 1 | Nov 1, 2013 | Genentech |
| NCT01967966 | Phase 1 | Nov 1, 2013 | Genentech |
| NCT01862081 | Phase 1 | Jul 16, 2013 | Genentech |
| NCT01814709 | Phase 1 | Apr 1, 2013 | Genentech |
| NCT01296555 | Phase 1 | Mar 16, 2011 | Genentech |
Showing 16 of 16 trials
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Organizations
Research & Development (19)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Genentech | For profit | 9 | 6 | 2 | 2011 |
| National Cancer Institute (NCI) | Government | 5 | 2 | 2 | 2014 |
| Roche | For profit | 3 | 1 | 3 | 2014 |
| ECOG-ACRIN Cancer Research Group | Academic/Hospital | 2 | 0 | 1 | 2015 |
| Southwest Oncology Group | Academic/Hospital | 2 | 2 | 2 | 2014 |
| Austrian Breast and Colorectal Cancer Group | Academic/Hospital | 1 | 0 | 1 | 2014 |
| Conquer Cancer Foundation | Academic/Hospital | 1 | 0 | 1 | 2015 |
| European Commission | Government | 1 | 0 | 1 | 2014 |
| Harvard University | Academic/Hospital | 1 | 1 | 1 | 2015 |
| Netherlands Cancer Institute | Academic/Hospital | 1 | 1 | 1 | 2014 |
| Pfizer | For profit | 1 | 0 | 1 | 2015 |
| Royal Marsden Hospital NHS Trust | Academic/Hospital | 1 | 1 | 1 | 2015 |
| SOLTI Breast Cancer Research Group | Academic/Hospital | 1 | 0 | 1 | 2014 |
| University of Amsterdam | Academic/Hospital | 1 | 0 | 1 | 2014 |
| University of Burgundy | Academic/Hospital | 1 | 1 | 1 | 2017 |
| University of Cambridge | Academic/Hospital | 1 | 0 | 1 | 2014 |
| University of London | Academic/Hospital | 1 | 0 | 1 | 2015 |
| University of Milan | Academic/Hospital | 1 | 0 | 1 | 2014 |
| Vanderbilt University | Academic/Hospital | 1 | 1 | 1 | 2015 |
19 organizations
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