Drug name
Last update: Jan 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
Not provided
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 technologies
Not provided
Comment & 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
No proprietary excipient used
Not provided
Not provided
Delivery device(s)
No delivery device
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 EP and CN
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
Publications
Chang, Y. S., Li, S. Y., Pertinez, H., Betoudji, F., Lee, J., Rannard, S. P., Owen, A., Nuermberger, E. L., & Ammerman, N. C. (2023). Using dynamic oral dosing of rifapentine and rifabutin to simulate exposure profiles of long-acting formulations in a mouse model of tuberculosis preventive therapy. bioRxiv : the preprint server for biology, 2023.04.12.536604. https://doi.org/10.1101/2023.04.12.536604
Administration of tuberculosis preventive therapy (TPT) to individuals with latent tuberculosis infection is an important facet of global tuberculosis control. The use of long-acting injectable (LAI) drug formulations may simplify and shorten regimens for this indication. Rifapentine and rifabutin have anti-tuberculosis activity and physiochemical properties suitable for LAI formulation, but there are limited data available for determining the target exposure profiles required for efficacy in TPT regimens. The objective of this study was to determine exposure-activity profiles of rifapentine and rifabutin to inform development of LAI formulations for TPT. We utilized a validated paucibacillary mouse model of TPT in combination with dynamic oral dosing of both drugs to simulate and understand exposure-activity relationships to inform posology for future LAI formulations. This work identified several LAI-like exposure profiles of rifapentine and rifabutin that, if achieved by LAI formulations, could be efficacious as TPT regimens and thus can serve as experimentally-determined targets for novel LAI formulations of these drugs. We present novel methodology to understand the exposure-response relationship and inform the value proposition for investment in development of LAI formulations that has utility beyond latent tuberculosis infection.
Additional documents
Useful links
There are no additional links
Collaborate for development
Consider on a case by case basis, collaborating on developing long acting products with potential significant public health impact, especially for low- and middle-income countries (LMICs), utilising the referred to long-acting technology
Share technical information for match-making assessment
Provide necessary technical information to a potential partner, under confidentiality agreement, to enable preliminary assessment of whether specific medicines of public health importance in LMICs might be compatible with the referred to long-acting technology to achieve a public health benefit
Work with MPP to expand access in LMICs
In the event that a product using the referred to long-acting technology is successfully developed, the technology IP holder(s) will work with the Medicines Patent Pool towards putting in place the most appropriate strategy for timely and affordable access in low and middle-income countries, including through licensing