DDInter1042 DDInter786
Leuprolide is a synthetic 9-residue peptide analogue of gonadotropin-releasing hormone (GnRH). Unlike the endogenous decapeptide GnRH, leuprolide contains a single D-amino acid (D-leucyl) residue, which helps to increase its circulating half-life from three to four minutes to approximately three hours. As a GnRH mimic, leuprolide is capable of binding to the GnRH receptor (GnRHR) and inducing downstream modulation of both gonadotropin hormone and sex steroid levels. Prolonged activation of GnRHR results in significant downregulation of sex steroid levels, which is primarily responsible for the clinical efficacy of leuprolide in diverse conditions, including advanced prostate cancer, endometriosis, and central precocious puberty.[A203126, A203132] Leuprolide was first approved in 1985 as a daily subcutaneous injection under the tradename
Fostemsavir is the phosphonooxymethyl prodrug of temsavir, a novel HIV-1 attachment inhibitor. It binds to and inhibits the activity of gp120, a subunit within the HIV-1 gp160 envelope glycoprotein that facilitates the attachment of HIV-1 to host cell CD4 receptors - in doing so, temsavir prevents the first step in the HIV-1 viral lifecycle. The discovery of gp120 as a potential target of interest in the treatment of HIV-1 infection is relatively recent, and was born out of a desire to find alternative target proteins (i.e. mechanistically orthogonal therapies) for the treatment of HIV-1 patients with resistant infections. Fostemavir is the first attachment inhibitor to receive FDA approval, granted in July 2020 for use in combination with other antiretrovirals in highly treatment-experienced patients with multidrug-resistant HIV-1 infection whom are failing their current therapy.[L14867,L14917] Targeting gp120 subunits is a new and novel therapeutic approach to HIV-1 infection, and the addition of attachment inhibitors, like temsavir, to the armament of therapies targeted against HIV-1 fills a necessary niche for therapeutic options in patients left with few, if any, viable treatments.
Fostemsavir {u} may cause a minor interaction that can limit clinical effects when taken with {v} Aminoglutethimide
Fostemsavir {u} may cause a minor interaction that can limit clinical effects when taken with {v} Brigatinib
Fostemsavir {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Quinine
Fostemsavir {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Triclabendazole
Fostemsavir {u} may lead to a major life threatening interaction when taken with {v} Ribociclib
Fostemsavir {u} may lead to a major life threatening interaction when taken with {v} Macimorelin
Fostemsavir may cause a minor interaction that can limit clinical effects when taken with Aminoglutethimide
Fostemsavir may cause a minor interaction that can limit clinical effects when taken with Brigatinib
Fostemsavir may cause a moderate interaction that could exacerbate diseases when taken with Quinine
Fostemsavir may cause a moderate interaction that could exacerbate diseases when taken with Triclabendazole
Fostemsavir may lead to a major life threatening interaction when taken with Ribociclib
Fostemsavir may lead to a major life threatening interaction when taken with Macimorelin