pictilisib

Small moleculeexperimental

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

Phase 1
13
Phase 2
4
Phase 3
0
Phase 4
0

Earliest trial started Oct 1, 2007 (NCT00876109)

Timeline

2000s

  1. Jan 1, 2007

    Earliest Phase 1 Sponsor(trial)

2010s

  1. Jan 1, 2011

    Earliest Phase 2 Sponsor(trial)

Indications

Mechanism of action

Chemistry & pharmacology

Loading structure…

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

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 IDPhaseStart dateSponsor(s)
NCT02389842Phase 1Feb 1, 2015Pfizer, Roche, Royal Marsden Hospital NHS Trust, University of London
NCT02092831Phase 1Apr 1, 2014Genentech, Roche
NCT01918306Phase 1/Phase 2 (Phase 2)Sep 1, 2013Genentech, National Cancer Institute (NCI), Vanderbilt University
NCT01740336Phase 2Feb 6, 2013Genentech
NCT01493843Phase 2Jan 20, 2012Genentech, Roche
NCT01437566Phase 2Oct 1, 2011Genentech
NCT01474668Phase 1Oct 1, 2011Genentech
NCT01240226Phase 1Nov 1, 2010Genentech
NCT00996892Phase 1Nov 1, 2009Genentech
NCT00999128Phase 1Oct 26, 2009Genentech
NCT00974584Phase 1Oct 1, 2009Genentech
NCT00975182Phase 1Sep 1, 2009Genentech
NCT00960960Phase 1Aug 1, 2009Genentech
NCT00928330Phase 1Jul 1, 2009Genentech
NCT00876122Phase 1Mar 1, 2008Genentech
NCT00876109Phase 1Oct 1, 2007Genentech
Showing 16 of 16 trials
Page 1 / 1

Organizations

Research & Development (7)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
GenentechFor profit151422007
RocheFor profit3022012
National Cancer Institute (NCI)Government1012013
PfizerFor profit1012015
Royal Marsden Hospital NHS TrustAcademic/Hospital1112015
University of LondonAcademic/Hospital1012015
Vanderbilt UniversityAcademic/Hospital1112013
7 organizations
Page 1 / 1