Abstract:Rifamycins are considered a milestone for tuberculosis (TB) treatment because of their proficient sterilizing ability. Currently, available TB treatments are complicated and need a long duration, which ultimately leads to failure of patient compliance. Some new rifamycin derivatives, i.e., rifametane, TNP-2092 (rifamycin-quinolizinonehybrid), and TNP-2198 (rifamycin-nitromidazole hybrid) are under clinical trials, which are attempting to overcome the problems associated with TB treatment. The undertaken review is intended to compare the pharmacokinetics, pharmacodynamics and safety profiles of these rifamycins, including rifalazil, another derivative terminated in phase II trials, and already approved rifamycins. The emerging resistance of microbes is an imperative consideration associated with antibiotics. Resistance development potential of microbial strains against rifamycins and an overview of chemistry, as well as structure-activity relationship (SAR) of rifamycins, are briefly described. Moreover, issues associated with rifamycins are discussed as well. We expect that newly emerging rifamycins shall appear as potential tools for TB treatment in the near future.

01 Jan 1999·ChemotherapyQ4 · MEDICINE

Phase I Pharmacokinetic Study of a New 3-Azinomethyl-Rifamycin (Rifametane) as Compared to Rifampicin

Q4 · MEDICINE

Article

Author: Potkar, C. ; Ajay, S. ; Shirsagar, N. A. ; Cooverji, N. D. ; Bruzzese, T. ; Gogtay, N. ; Gokhale, P.

An open randomized cross-over study was conducted in 8 healthy male volunteers to study the pharmacokinetic pattern and the safety of a 300-mg single oral dose of a new 3-azinomethyl-rifamycin (USAN rifametane, SPA-S-565) compared with 300 mg of conventional rifampicin. The pharmacokinetic profiles of rifametane were significantly more favorable than those of rifampicin. The serum peak value was 7.82 µg/ml for rifametane and 4.04 µg/ml for rifampicin (p < 0.001); the elimination half-life was 10.58 h for rifametane and 1.89 h for rifampicin (p < 0.001); area under the serum concentration curve from 0 to infinity was 142.3 µg·h/ml for rifametane and 19.9 µg·h/ml for rifampicin (p < 0.001); the mean residence time was 18.05 h for rifametane and 3.93 h for rifampicin (p < 0.001). Rifametane showed a good safety profile after the 300-mg single oral dose. Three volunteers developed a mild headache, metallic taste and slightly elevated temperature for 3–4 h, which subsided without medication. Clinically or statistically significant changes in laboratory parameters were not found between baseline and posttreatment values.

01 Dec 1998·Nihon rinsho. Japanese journal of clinical medicine

[Chemotherapeutic agents under study].

Review

Author: Kawahara, S

The development of new drugs with strong antituberculous activity and fewer side effects which are not cross-resistant to conventional antituberculosis drugs is urgently desired now. The chemotherapeutic agents under study which are considered a candidate for a new antituberculosis drug are listed below. 1) Rifamycin derivatives: rifabutin, rifapentin, KRM-1648, FCE-22250, 22807, CGP-7040, 27557, 29035, 29861, P-DEA, SPA-S-565, R-76-1. 2) New quinolones: ofloxacin, ciprofloxacin, levofloxacin, sparfloxacin, gatifloxacin, CS-940, Du-6859a. 3) Phenazines: clofazimine, B746, B4101, B4154, B4157. 4) Pyrazinamide derivatives: N-hydroxy pyrazinamide, N-hydroxy pyrazinamide-4-oxide. 5) Nitroimidazole derivatives: metronidazole et al.

100 Deals associated with Rifametane

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Indication	Highest Phase	Country/Location	Organization	Date
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Bacterial Infections	Phase 1	-	Novartis Pharma AG	-

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