Article · Wikipedia archive · Last revised Aug 5, 2026

Ipatasertib

Ipatasertib (RG7440) is an experimental cancer drug in development by Roche. It is a small molecule inhibitor of AKT, which is a key component of the PI3K/AKT pathway. Ipatasertib was discovered by Genentech in collaboration with Array Biopharma and is currently in phase III trials for treatment of breast cancer.

Last revised
Aug 5, 2026
Read time
≈ 1 min
Length
157 w
Citations
2
Source
Wikipedia ↗
Ipatasertib
Clinical data
Routes of
administration		PO
ATC code
  • None
Identifiers
  • (S)-2-(4-Chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one
CAS Number
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC24H32ClN5O2
Molar mass458.00 g·mol−1
3D model (JSmol)
  • CC(C)NC[C@@H](C(=O)N1CCN(CC1)C1=C2[C@H](C)C[C@@H](O)C2=NC=N1)C1=CC=C(Cl)C=C1
  • InChI=1S/C24H32ClN5O2/c1-15(2)26-13-19(17-4-6-18(25)7-5-17)24(32)30-10-8-29(9-11-30)23-21-16(3)12-20(31)22(21)27-14-28-23/h4-7,14-16,19-20,26,31H,8-13H2,1-3H3/t16-,19-,20-/m1/s1
  • Key:GRZXWCHAXNAUHY-NSISKUIASA-N

Ipatasertib (RG7440) is an experimental cancer drug in development by Roche. It is a small molecule inhibitor of AKT, which is a key component of the PI3K/AKT pathway. Ipatasertib was discovered by Genentech in collaboration with Array Biopharma and is currently in phase III trials for treatment of breast cancer.1

In vitro, ipatasertib showed activity against all three isoforms of Akt.2

References

References

  1. Clinical trial number NCT02301988 for "A Study of Ipatasertib (GDC-0068) in Combination With Paclitaxel as Neoadjuvant Treatment for Participants With Early Stage Triple Negative Breast Cancer" at ClinicalTrials.gov
  2. Lin J, Sampath D, Nannini MA, Lee BB, Degtyarev M, Oeh J, et al. (April 2013). "Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models". Clinical Cancer Research. 19 (7): 1760–72. doi:10.1158/1078-0432.CCR-12-3072. PMID 23287563.