Drug name
Last update: Jul 2026Depulfavirine nanosphere LAI
Developer(s)
Drug information
Depulfavirine; VM-1500A-LAI
Depulfavirine
Small molecule
Diphenylether Non-nucleoside reverse transcriptase Allosteric inhibitor
Depulfavirine (VM1500A) is a second-generation allosteric non-nucleoside reverse transcriptase inhibitor (NNRTI). Its prodrug, elsulfavirine (ESV), has been authorised for the treatment of HIV-1 infection in several Eurasian countries as a once-daily oral regimen and has demonstrated favourable antiviral efficacy. Depulfavirine is currently under evaluation in Phase II/III clinical trials (NCT05204394) conducted in Russia. Pharmacokinetic studies indicate that depulfavirine exhibits a prolonged elimination half-life of approximately 5.4–7.4 days. Furthermore, crystalline or polycrystalline nanoparticle formulations (200–900 nm) have been developed for long-acting injectable delivery. In vitro studies have shown potent antiviral activity, with IC₅₀ values for VM1500A against wild-type HIV-1
Under clinical investigation and not approved yet
Under clinical investigation and not approved yet
Therapeutic area(s)
- HIV
- Treatment
Administration route
Intramuscular
Associated long-acting platforms
nanosphere
Use of drug
- Administered by a community health worker
- Administered by a nurse
- Administered by a specialty health worker
- Monthly
Dosage
600 mg; 900 mg IM
900 mg IM
1. Depulfavirine [VM-1500A-LAI] 600mg IM Q4W with the oral-lead 2 NRTIs daily. 2. Depulfavirine [VM-1500A-LAI] 900mg IM Q4W with the oral-lead 2 NRTIs daily
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Associated compounds, formulations and regimens
Not provided
Associated technologies
Not provided
Additional information
Developer(s)
Viriom
Viriom Inc. is a commercial-stage biotechnology firm that focuses on creating and marketing high-efficacy, reasonably priced treatments for cancer and infectious disorders. Viriom Inc. was founded in 2009 as a spin-out of the Russian R&D group ChemRar High Tech Center. Viriom was created especially to create HIV/AIDS-specific medications. It launched by licensing Hoffmann-La Roche drugs.
Drug structure
Scale-up and manufacturing prospects
Not provided
1. Rotary jar mill (U.S. Stoneware 700 Series Jar Mill) 2. Grinding jars (milling jars) 3. Zirconia grinding media (Zircon Sand) - 0.5 mm YTZ® Zirconia grinding and dispersion media 4. Refrigerated storage 5. Filtration apparatus 6. Particle size analyzer (Malvern Zetasizer Nano ZS)
Manufacturing process and considerations: 1. Aqueous solution containing poloxamer + saccharide 2. Add Crystalline Depulfavirine in the aqueous phase 3. Wet Nanomelling with zirconia for 24 h at ~104 rpm 3. Settling: 16–20 h at 2–8 °C 4. Lyophilisation of nanosuspension forming stable dry nanospore cake 5. Filtration to remove grinding media 5. Freeze drying and reconstitution
1. HPLC–MS/MS System
Excipients & delivery device(s)
Not provided
1. Poloxamer P338 2. Mannitol or saccharose 3. Phosphate buffered saline (PBS), water for injection
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No delivery device
Safety, Efficacy and Evidence Summary
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PHARMACEUTICAL NANOSUSPENSION FOR THE THERAPY OF HIV INFECTION
The present invention relates to a pharmaceutical composition (nanosuspension) for a long-acting injectable (LAI) drug for the long-term maintenance therapy of HIV/AIDS. A pharmaceutical nanosuspension for use as an injectable drug for the long-term maintenance therapy of HIV infection is claimed, comprising a composition that contains, as an active ingredient, a compound of general formula 1 in crystalline or polycrystalline form, in which R is C2H5CON-Na+, NH2.
EP3643304A1
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VIRIOM INC
Not provided
February 14, 2038
Anticipated expiration
Substituted 3,4,12,12a-Tetrahydro-1H-[1,4]Oxazino[3,4-c]Pyrido[2,1-f][1,2,4]Triazine-6,8-dione, Pharmaceutical Composition, Method for the Production and Use Thereof
Substituted 3,4,12,12a-tetrahydro-1H-[1,4]-oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione of general formula 1, its stereoisomer, their prodrug, pharmaceutically acceptable salt, solvate, hydrate, and a crystalline or polycrystalline form thereofwhere:R1 is diphenylmethyl, bis(4-fluorophenyl)methyl, (3,4-difluorophenyl)(phenyl)methyl, (3,4-difluorophenyl)(2-methylsulfanylphenyl)methyl;R2 is hydrogen or a {[(C1-C3alkyl)oxycarbonyl]-oxy}methoxy and stereoisomers thereof.
US20240383919A1
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Viriom Inc
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Pending