Ipatasertib

(GDC-0068, RG7440)

Breast
  • Phase
  • III
  • II
  • I
Gastrointestinal
  • Phase
  • III
  • II
  • I
Genitourinary
  • Phase
  • III
  • II
  • I
Gynecologic
  • Phase
  • III
  • II
  • I
Hematologic
  • Phase
  • III
  • II
  • I
Lung
  • Phase
  • III
  • II
  • I
Melanoma
  • Phase
  • III
  • II
  • I
Solid Tumor
  • Phase
  • III
  • II
  • I

This compound and its uses are investigational and have not been approved by the US Food and Drug Administration. Efficacy and safety have not been established. The information presented should not be construed as a recommendation for use. The relevance of findings in preclinical studies to humans is currently being evaluated.

Ipatasertib, an Akt inhibitor

Ipatasertib, an investigational Akt inhibitor, is currently in clinical development based on its potential to specifically target Akt in tumors with activated Akt signaling. Preclinical data have shown that ipatasertib selectively decreased cell viability and increased apoptosis in tumor cell lines characterized by activated Akt.1,2 Ipatasertib continues to be investigated in ongoing clinical studies.

1 Ipatasertib (GDC-0068) is an investigational small-molecule inhibitor currently being studied for its potential to selectively bind to all 3 isoforms of Akt.1,2

Ipatasertib image: an investigational Akt inhibitor currently being studied for its potential to selectively bind to all 3 Akt isoforms

 

2 Ipatasertib is designed to target and bind to the ATP-binding pocket of the 3 isoforms of Akt, potentially inhibiting downstream signaling.1,2

Ipatasertib image: designed to target and bind to Akt isoforms, which may inhibit downstream signaling

 

3 Preclinical data have shown that ipatasertib induced tumor growth delay or regression in Akt activated tumor cell xenograft models.1 Ipatasertib continues to be investigated in ongoing clinical studies.

Ipatasertib image: ipatasertib induced tumor growth delay or regression in Akt activated tumor cell xenograft models

References

  1. Lin J, Sampath D, Nannini MA, et al. Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Cancer Res. 2013;19:1760-1772. doi:10.1158/1078-0432.ccr-12-3072. PMID: 23287563
  2. Yan Y, Serra V, Prudkin L, et al. Evaluation and clinical analyses of downstream targets of the Akt inhibitor GDC-0068. Clin Cancer Res. 2013;19:6976-6986. PMID: 24141624