Drug name
Last update: Jun 2026Rifapentine LAI
Developer(s)
Drug information
Rifapentine solid drug nanoparticle
Not provided
Small molecule
Not provided
Intramuscular administration of rifapentine as a solid drug nanoparticle (SDN) suspension at weekly doses of 187.5 and 375 mg/kg produced a pharmacokinetic profile comparable to that observed with oral risperidone formulations. Preclinical evaluations demonstrated dose-dependent pharmacokinetics, with estimated release rate constants ranging from 0.0015 to 0.0025 h⁻¹. The AUC1-14d values were 6.629 and 13.071 µg·h/L for the 187.5 and 375 mg/kg doses, respectively. Physiologically based pharmacokinetic (PBPK) modeling further indicated a cumulative 11% increase in apparent clearance per dosing day following repeated administration of rifapentine SDN.
Not approved yet.
Not approved yet.
Therapeutic area(s)
- TB
- Prevention
Administration route
Intramuscular
Associated long-acting platforms
Solid Drug Nanoparticle suspension
Use of drug
- Administered by a community health worker
- Administered by a nurse
- Administered by a specialty health worker
- Every 2 weeks
- Monthly
Dosage
Animal dosage tested: 46.9 mg/kg; 93.75 mg/kg; 187.5 mg/kg; and 375 mg/kg IM
Animal Maximum dose tested: 375 mg/kg IM
Not provided
Not provided
Associated compounds, formulations and regimens
Not provided
Associated technologies
Not provided
Additional information
Developer(s)
Centre for Excellence of Long-acting Therapeutics
The Centre of Excellence for Long-acting Therapeutics (CELT) is a cross-faculty research initiative combining our world leading expertise in pharmacology and materials chemistry and working with international partners to disseminate research findings in long-acting medicine and change the global landscape of drug administration.
Drug structure
Scale-up and manufacturing prospects
Not provided
Not provided
Not provided
Not provided
Excipients & delivery device(s)
No proprietary excipient used
Not provided
Not provided
No delivery device
Safety, Efficacy and Evidence Summary
Not provided
Not provided
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Solid compositions comprising nanoparticles of Rifapentine
he present invention relates to solid compositions comprising nanoparticles of a Rifamycin, such a Rifapentine, dispersed within a matrix comprising a first excipient and a second excipient. The present invention also relates to microneedle arrays, implantable rods, aqueous dispersions, and pharmaceutical compositions derived from said solid compositions and uses for the same. In the method of the sixteenth aspect of the present invention, the concentration of the Rifamycin, such as Rifapentine, within the aqueous dispersion, the pharmaceutical composition, or the injectable formulation may be 100 to 1000 mg/mL, preferably 200 to 900 mg/mL, more preferably 300 to 800 mg/mL, and most preferably 500 to 700 mg/mL.
WO2024194655
Formulation
THE UNIVERSITY OF LIVERPOOL
Not provided
March 22, 2044
Pending in CN, IN, EP and US
Rifapentine compound and preparation process
ovel rifamycin SV derivatives of the general Formula I wherein R is cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl, each optionally substituted once or twice by methyl and/or ethyl, are prepared by contacting 3-formylrifamycin SV with 1-1.1 molar equivalents of an aminopiperazine of the general Formula II in the presence of an inert organic solvent at from ambient temperature to the reflux temperature of the reaction mixture. Pharmaceutical compositions having antibacterial activity comprise, as active ingredient, a rifamycin derivative of the general Formula a I, together with a pharmaceutically acceptable carrier.
US4002752
Compound
LEPETIT SPA
Not provided
March 5, 1995
Expired