apitolisib
Small moleculeexperimental
Clinical trial activity
12 trials · 1 clinical orgs · 0 marketing orgs
Phase 1
9
Phase 2
4
Phase 3
0
Phase 4
0
Earliest trial started Mar 1, 2009 (NCT00854152)
Timeline
Indications
Mechanism of action
- Serine/threonine-protein kinase mTORINHIBITOR
MTOR inhibitor
Dual MTOR/PIK3 inhibitor, ATP-competitive mTORC1/mTORC2 inhibitor
- PI3-kinase class IINHIBITOR
PI3-kinase class I inhibitor
Dual MTOR/PIK3 inhibitor, ATP-competitive mTORC1/mTORC2 inhibitor
- 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
Cc1c(CN2CCN(C(=O)[C@H](C)O)CC2)sc2c(N3CCOCC3)nc(-c3cnc(N)nc3)nc12- Mol. weight
- 498.61 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL1922094 ↗
Also known as
- 1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno(3,2-d)pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one
- apitolisib
- apitolisib
- apitolisib
- g-038390
- g-038390
- g-038390.1
- g-038390.1
- gdc0980
- gdc 0980
- gdc-0980
- gdc-0980
- gdc-0980
- gdc-0980
- gdc-0980.1
- gdc-0980.1
- rg-7422
- rg-7422
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT01485861 | Phase 1/Phase 2 (Phase 2) | Jan 11, 2012 | Genentech |
| NCT01455493 | Phase 2 | Dec 1, 2011 | Genentech |
| NCT01487239 | Phase 1 | Dec 1, 2011 | Genentech |
| NCT01473316 | Phase 1 | Nov 1, 2011 | Genentech |
| NCT01437566 | Phase 2 | Oct 1, 2011 | Genentech |
| NCT01442090 | Phase 2 | Oct 1, 2011 | Genentech |
| NCT01301716 | Phase 1 | Sep 1, 2011 | Genentech |
| NCT01332604 | Phase 1 | Jul 1, 2011 | Genentech |
| NCT01254526 | Phase 1 | Dec 1, 2010 | Genentech |
| NCT01287091 | Phase 1 | Oct 1, 2010 | Genentech |
| NCT00854126 | Phase 1 | May 1, 2009 | Genentech |
| NCT00854152 | Phase 1 | Mar 1, 2009 | Genentech |
Showing 12 of 12 trials
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Organizations
Research & Development (1)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Genentech | For profit | 12 | 12 | 2 | 2009 |
1 organizations
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