On November 16, 2023, Bristol Myers Squibb announced that the U.S. Food and Drug Administration (FDA) has approved ripretinib (Augtyro) for the treatment of adult patients with locally advanced or metastatic ROS1-positive non-small cell lung cancer (NSCLC). As an oral therapy, ripretinib (Augtyro) is a tyrosine kinase inhibitor (TKI) that targets ROS1 oncogenic fusions.
“Despite the progress made in the treatment of non-small cell lung cancer over the past decade, there remains a need to address this particularly difficult-to-treat form of disease through innovative science and targeted approaches,” said Samit Hirawat, MD, Executive Vice President and Chief Medical Officer of Global Drug Development at Bristol Myers Squibb. “As the only approved next-generation TKI for patients with ROS1-positive non-small cell lung cancer, ripretinib (Augtyro) continues our tradition of providing transformative therapies for patients with thoracic tumors.”
“Patients with ROS1-positive non-small cell lung cancer and their families are going through a stressful journey because this cancer is difficult to treat, especially when it spreads to the brain,” said Janet Freeman-Daily, co-founder and president of the patient advocacy group TheROS1ders. “Today’s approval brings a new treatment option to the ROS1-positive patient community, giving us hope to spend more time with our loved ones.”
Ripretinib (Augtyro) Indications
Ripretinib (Augtyro) is indicated for the treatment of adult patients with locally advanced or metastatic ROS1-positive non-small cell lung cancer (NSCLC).
Ripretinib (Augtyro) Drug Interactions
Effects of Other Drugs on Ripretinib
Potential and Intermediate CYP3A Inhibitors
Concomitant use with potent or intermediate CYP3A inhibitors should be avoided. Concomitant use of ripretinib with potent or intermediate CYP3A inhibitors may increase the risk of complications. Increased exposure to ripretinib may increase the incidence and severity of adverse reactions. Before initiating ripretinib, CYP3A inhibitors should be discontinued for 3 to 5 elimination half-lives of the CYP3A inhibitor.
P-glycoprotein (P-gp) inhibitors
Concomitant use with P-glycoprotein inhibitors should be avoided. Concomitant use of ripretinib with P-glycoprotein inhibitors may increase ripretinib exposure, potentially increasing the incidence and severity of adverse reactions.
Potential and intermediate-potency CYP 3A Inducers
Concomitant use with potent or intermediate-potency CYP3A inducers should be avoided. Concomitant use of ripretinib with potent or intermediate-potency CYP3A inducers may decrease ripretinib plasma concentrations, potentially reducing the efficacy of ozogitiro.
Effects of Ripretinib (Augtyro) on Other Drugs
Specific CYP3A4 Substrates
Concomitant use should be avoided unless otherwise recommended in the CYP3A substrate prescribing information (i.e., small changes in concentration may lead to reduced efficacy). If concomitant use cannot be avoided... The dosage of the CYP3A4 substrate should be increased according to the approved product instructions.
Riprotinib is a CYP3A4 inducer. Concomitant use of riprotinib with CYP3A4 substrates may reduce substrate concentrations, potentially decreasing the efficacy of these substrates.
Contraceptives
As a CYP3A4 inducer, riprotinib may reduce progestin or estrogen exposure, potentially reducing the effectiveness of hormonal contraceptives.
Concomitant use of riprotinib with hormonal contraceptives should be avoided. Women are advised to use effective non-hormonal contraceptive methods.
