pictilisib
Phosphoinositide 3-kinase inhibitors are a class of medical drugs that are mainly used to treat advanced cancers. They function by inhibiting one or more of the phosphoinositide 3-kinase (PI3K) enzymes, which are part of the PI3K/AKT/mTOR pathway. This signal pathway regulates cellular functions such as growth and survival. It is strictly regulated in healthy cells, but is always active in many cancer cells, allowing the cancer cells to better survive and multiply. PI3K inhibitors block the PI3K/AKT/mTOR pathway and thus slow down cancer growth. They are examples of a targeted therapy. While PI3K inhibitors are an effective treatment, they can have very severe side effects and are therefore only used if other treatments have failed or are not suitable. — Wikipedia
Clinical trial activity
16 trials · 7 clinical orgs · 0 marketing orgs
Earliest trial started Oct 1, 2007 (NCT00876109)
Timeline
Indications
Mechanism of action
- PI3-kinase class IINHIBITOR
PI3-kinase class I 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
SMILES
CS(=O)(=O)N1CCN(Cc2cc3nc(-c4cccc5[nH]ncc45)nc(N4CCOCC4)c3s2)CC1- Mol. weight
- 513.65 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaPhosphoinositide 3-kinase inhibitor ↗
- ChEMBLCHEMBL521851 ↗
Also known as
- 2-(1h-indazol-4-yl)-6-(4-methanesulfonylpiperazin-1-ylmethyl)-4-morpholin-4-ylthieno(3,2-d)pyrimidine
- gdc0941
- gdc 0941
- gdc-0941
- gdc-0941
- gdc-0941
- gdc-0941
- pictilisib
- pictilisib
- pictilisib
- pictilisib
- rg-7321
- rg-7321
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02389842 | Phase 1 | Feb 1, 2015 | Pfizer, Roche, Royal Marsden Hospital NHS Trust, University of London |
| NCT02092831 | Phase 1 | Apr 1, 2014 | Genentech, Roche |
| NCT01918306 | Phase 1/Phase 2 (Phase 2) | Sep 1, 2013 | Genentech, National Cancer Institute (NCI), Vanderbilt University |
| NCT01740336 | Phase 2 | Feb 6, 2013 | Genentech |
| NCT01493843 | Phase 2 | Jan 20, 2012 | Genentech, Roche |
| NCT01437566 | Phase 2 | Oct 1, 2011 | Genentech |
| NCT01474668 | Phase 1 | Oct 1, 2011 | Genentech |
| NCT01240226 | Phase 1 | Nov 1, 2010 | Genentech |
| NCT00996892 | Phase 1 | Nov 1, 2009 | Genentech |
| NCT00999128 | Phase 1 | Oct 26, 2009 | Genentech |
| NCT00974584 | Phase 1 | Oct 1, 2009 | Genentech |
| NCT00975182 | Phase 1 | Sep 1, 2009 | Genentech |
| NCT00960960 | Phase 1 | Aug 1, 2009 | Genentech |
| NCT00928330 | Phase 1 | Jul 1, 2009 | Genentech |
| NCT00876122 | Phase 1 | Mar 1, 2008 | Genentech |
| NCT00876109 | Phase 1 | Oct 1, 2007 | Genentech |
Organizations
Research & Development (7)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Genentech | For profit | 15 | 14 | 2 | 2007 |
| Roche | For profit | 3 | 0 | 2 | 2012 |
| National Cancer Institute (NCI) | Government | 1 | 0 | 1 | 2013 |
| Pfizer | For profit | 1 | 0 | 1 | 2015 |
| Royal Marsden Hospital NHS Trust | Academic/Hospital | 1 | 1 | 1 | 2015 |
| University of London | Academic/Hospital | 1 | 0 | 1 | 2015 |
| Vanderbilt University | Academic/Hospital | 1 | 1 | 1 | 2013 |