Fostemsavir: First Approval
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ADISINSIGHT REPORT
Fostemsavir: First Approval Anthony Markham1
© Springer Nature Switzerland AG 2020
Abstract Fostemsavir (Rukobia), a prodrug of the HIV-1 attachment inhibitor temsavir, is a first-in-class treatment for HIV infection being developed by ViiV Healthcare. Based on the results of the phase III BRIGHTE trial fostemsavir was recently approved in the USA for the treatment of patients with HIV not able to be treated with other therapies. This article summarizes the milestones in the development of fostemsavir leading to this first approval.
Fostemsavir (Rukobia): Key points An HIV-1 attachment inhibitor is being developed by ViiV Healthcare for the treatment of HIV infection Received its first approval on 2 July 2020 in the USA Approved for use in adults with HIV who have tried multiple HIV medications and whose HIV infection cannot be successfully treated with other therapies because of resistance, intolerance or safety considerations
inhibits the interaction between the virus and cellular CD4 receptors, preventing attachment. Temsavir also inhibits gp120-dependent post-attachment steps required for viral entry into host CD4+ T cells. Fostemsavir was approved in the USA on 2 July 2020 for the treatment of HIV-1 infection in heavily treatment-experienced adults with multidrugresistant HIV-1 infection failing their current antiretroviral regimen due to resistance, intolerance, or safety considerations [1, 2] and is under regulatory review in the European union [3]. The recommended dosage of fostemsavir is 600 mg administered orally twice daily.
1.1 Company Agreements
1 Introduction Fostemsavir (Rukobia), a prodrug of the HIV-1 attachment inhibitor temsavir, is a first-in-class treatment for HIV infection being developed by the specialized HIV company ViiV Healthcare. Temsavir binds directly to the glycoprotein (gp) 120 subunit within the HIV-1 envelope and selectively Enhanced material for this AdisInsight Report can be found at https://doi.org/10.6084/m9.figshare.12792599. This profile has been extracted and modified from the AdisInsight database. AdisInsight tracks drug development worldwide through the entire development process, from discovery, through preclinical and clinical studies to market launch and beyond. * Anthony Markham [email protected] 1
Springer Nature, Mairangi Bay, Private Bag 65901, Auckland 0754, New Zealand
In February 2016, ViiV Healthcare, a specialized HIV company established in late 2009 by GSK and Pfizer, acquired the HIV R&D portfolio of Bristol-Myers Squibb, which included fostemsavir [4].
2 Scientific Summary 2.1 Pharmacodynamics Temsavir neutralized BG505 pseudoviruses in vitro with half-maximal inhibitory concentrations ( IC50s) of 14 nmol/L against BG505 and BG505 T332N. Temsavir bound to a soluble version of the prefusion Env trimer BG505 SOSIP with a Kd of 73 nmol/L and the stabilized version DS-SOSIP with a Kd of 87 nmol/L. Soaking temsavir into crystals of the HIV-1 Env trimer comprising trimeric BG505 SOSIP bound by PGT122 (a 332-glycan dependent anti
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