Drug Overview
Ipatasertib (Roche) is a highly selective, ATP-competitive Akt inhibitor that preferentially targets active, phosphorylated Akt. Akt is dysregulated in a number of malignancies through loss of the tumor suppressor phosphatase and tensin homolog (PTEN), acquisition of activating mutations in phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha (PIK3CA) or AKT1, as well as amplification of PI3K. Additionally, signaling in the Pl3K/Akt/mTOR pathway has been shown to increase following antihormonal therapy or chemotherapy, which are standard regimens within the prostate cancer treatment paradigm.
Roche is investigating ipatasertib as part of a combination with Zytiga (abiraterone acetate; Johnson & Johnson/AstraZeneca) in asymptomatic or mildly symptomatic, previously untreated metastatic castration-resistant prostate cancer patients. Late-phase data are needed to determine the potential of ipatasertib in this indication, but targeting the PI3K/Akt/mammalian target of rapamycin (mTOR) pathway is a novel approach, and, if viable, could lead to further division of the prostate cancer treatment paradigm to include targeting patients with PI3K/Akt/mTOR abnormalities. Additionally, the success of Zytiga could be used to leverage the uptake of ipatasertib, but the combination will have to demonstrate strong efficacy and tolerability in order to justify its probable high price tag.
Ipatasertib (Roche) is a highly selective, ATP-competitive Akt inhibitor that preferentially targets active, phosphorylated Akt. Akt is dysregulated in a number of malignancies through loss of the tumor suppressor phosphatase and tensin homolog (PTEN), acquisition of activating mutations in phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha (PIK3CA) or AKT1, as well as amplification of PI3K. Additionally, signaling in the Pl3K/Akt/mTOR pathway has been shown to increase following antihormonal therapy or chemotherapy, which are standard regimens within the prostate cancer treatment paradigm.
Roche is investigating ipatasertib as part of a combination with Zytiga (abiraterone acetate; Johnson & Johnson/AstraZeneca) in asymptomatic or mildly symptomatic, previously untreated metastatic castration-resistant prostate cancer patients. Late-phase data are needed to determine the potential of ipatasertib in this indication, but targeting the PI3K/Akt/mammalian target of rapamycin (mTOR) pathway is a novel approach, and, if viable, could lead to further division of the prostate cancer treatment paradigm to include targeting patients with PI3K/Akt/mTOR abnormalities. Additionally, the success of Zytiga could be used to leverage the uptake of ipatasertib, but the combination will have to demonstrate strong efficacy and tolerability in order to justify its probable high price tag.
Table of Contents
Product Profilesipatasertib: Prostate cancer
List of Figures
Figure 1: Ipatasertib for prostate cancer - SWOT analysis
Figure 2: Drug assessment summary of ipatasertib for prostate cancer
Figure 3: Drug assessment summary of ipatasertib for prostate cancer
Figure 4: Ipatasertib sales for prostate cancer across the US, Japan, and five major EU markets, by country, 2017-26
List of Tables
Table 1: Ipatasertib drug profile
Table 2: Ipatasertib Phase III trial in prostate cancer
Table 3: Ipatasertib Phase II data in prostate cancer
Table 4: Ipatasertib sales for prostate cancer across the US, Japan, and five major EU markets, by country ($m), 2017-26
