Taselisib

(GDC-0032, RG7604)

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.

Taselisib, a PI3K inhibitor

Taselisib, an investigational PI3K inhibitor, is currently in clinical development based on its potential selectivity for the PI3Kα isoform.1,2 Preclinical data have shown that taselisib induced growth inhibition in PI3Kα-mutant cell lines.1 Taselisib continues to be investigated in ongoing clinical studies.

1 Taselisib is an investigational PI3K inhibitor currently being studied for its potential to selectively inhibit the PI3Kα isoform.1,2

 

2 Taselisib is designed to bind to the ATP-binding pocket of PI3Kα to potentially prevent subsequent downstream signaling.1

 

3 In preclinical studies, taselisib induced growth inhibition in PI3Kα-mutant xenograft mouse models.1 Taselisib continues to be investigated in ongoing clinical studies.

References

  1. Lopez S, Schwab CL, Cocco E, et al. Taselisib, a selective inhibitor of PIK3CA, is highly effective on PIK3CA-mutated and HER2/neu amplified uterine serous carcinoma in vitro and in vivo. Gynecol Oncol. 2014;135:312-317. PMID: 25172762
  2. Ndubaku CO, Heffron TP, Staben ST, et al. Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity. J Med Chem. 2013;56:4597-4610. PMID: 23662903