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Rukobia
Published
Product name
Rukobia
Active ingredient
Fostemsavir trometamol
Submission type
New chemical entity
Decision
Approved
Decision date
Registration date
What this medicine was approved for
Rukobia (fostemsavir trometamol) was approved for the following therapeutic use:
Rukobia is indicated in combination with other antiretroviral agents for the treatment of heavily treatment-experienced adults with multidrug-resistant human immunodeficiency virus-1 (HIV-1) infection for whom it is otherwise not possible to construct a suppressive antiviral regimen due to resistance, intolerance or safety considerations (see Section 5.1 Pharmacodynamic properties, clinical trials).
How this medicine works
Fostemsavir is a prodrug without significant biochemical or antiviral activity that is hydrolysed to the active moiety, temsavir, upon cleavage of a phosphonooxymethyl group in vivo. Temsavir binds directly to the glycoprotein (gp)120 subunit within the human immunodeficiency virus-1 (HIV-1) envelope glycoprotein gp160 and selectively inhibits the interaction between the virus and cellular cluster of differentiation 4 (CD4) receptors, thereby preventing viral entry into, and infection of, host cells. Temsavir inhibited the binding of soluble CD4 to surface immobilised gp120 with a half maximal inhibitory concentration (IC50) of 14 to 30 nM using an enzyme linked immunosorbent assay.
Why the TGA approved or did not approve this medicine
The decision was based on quality (chemistry and manufacturing), nonclinical (pharmacology and toxicology), clinical (pharmacology, safety and efficacy) and risk management plan information submitted by the sponsor. The benefit-risk profile of Rukobia was considered favourable for the therapeutic use approved.
Sponsor