Drug name
Last update: Jul 2025Rifabutin
Developer(s)
Drug information
Rifabutin
Mycobutin
Small molecule
Not provided
Rifabutin is a broad-spectrum antibiotic used for the treatment of tuberculosis (TB) and has applications as mycobacterium avium complex prophylaxis in HIV-positive individuals. Rifabutin displays a wide range of bactericidal activity and functions through the inhibition of the bacterial DNA-dependent RNA polymerase. Given concerns regarding potential antibiotic resistance, the prescribing of Rifabutin is often restricted to the treatment mycobacterium infection and other limited applications. Rifabutin is well tolerated when administered orally, and is readily distributed throughout the body including the cerebrospinal fluid. Long-acting injectable versions of Rifabutin are currently in development and could potentially transform TB prevention and treatment.
Unknown
Unknown
Therapeutic area(s)
- TB
- Pre-Exposure Prophylaxis (PrEP)
- Treatment
Administration route
Oral, Subcutaneous
Associated long-acting platforms
In-situ forming gel/implant
Use of drug
- Administered by a nurse
- Administered by a specialty health worker
Not provided
Dosage
Not provided
Not provided
Not provided
Not provided
Not provided
Associated compounds, formulations and regimens
Not provided
Associated technologies
Not provided
Additional information
Developer(s)
Pfizer
Pfizer is a multinational pharmaceutical company headquartered in Manhattan, New York, USA. Pfizer develops vaccines and medicines for therapeutic areas including neurology, immunology, Covid-19, endocrinology, cardiology and oncology. Rifabutin was originally discovered by the Italian pharma company Archifar in 1975, who were subsequently acquired by Pharmacia in 1980 and later by Pfizer in 2003.
Drug structure
Scale-up and manufacturing prospects
Formulations for long-acting Rifabutin are currently in the pre-clinical development stage, and therefore detailed scale-up information is not currently available. One promising formulation termed RFB14KH developed at the University of North Carolina, Chapel Hill contains several FDA-approved components utilised in existing in-situ forming implants, including Kolliphor®HS 15 (Macrogol (15)-hydroxystearate), DMSO and PLGA (poly(lactic-co-glycolic acid)).
Information regarding industrial processes and/or manufacturing equipment is currently not available as long-acting Rifabutin formulations have been only been produced at small-scale for research use.
The previously mentioned RFB14KH formulation developed by researchers at the University of North Carolina, Chapel Hill was stored at room temperature in the absence of light and maintained stability for 18 months.
HPLC and UV-Vis absorbance spectrometer for the evaluation of drug degradation and drug concentration. Zeiss Supra 25 field emission scanning electron microscope for characterisation of in-vitro implant formation.
Excipients & delivery device(s)
No proprietary excipient used
Not provided
Dimethyl sulfoxide (DMSO) which is a ICH Q3C class 3 solvent.
No delivery device
Safety, Efficacy and Evidence Summary
Not provided
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Not provided
Not provided
Rifamicyn compounds
Rifabutin compound
US4219478
Compound
Archifar Lab Chim Farm
Not provided
June 2, 1996
expired