A Phase 2 Trial to Evaluate the Early Bactericidal Activity, Safety and Tolerability of Sanfetrinem Cilexetil Administered Orally to Adults With Newly Diagnosed, Smear-Positive, Rifampicin-Susceptible Pulmonary Tuberculosis

To evaluate the 2-week bactericidal activity, pharmacokinetics, safety and tolerability of sanfetrinem cilexetil in participants with rifampicin-susceptible pulmonary tuberculosis.

Start Date21 Apr 2022

Sponsor / Collaborator

TASK Applied Science

[+1]

100 Clinical Results associated with Sanfetrinem cilexetil

100 Translational Medicine associated with Sanfetrinem cilexetil

100 Patents (Medical) associated with Sanfetrinem cilexetil

Literatures (Medical) associated with Sanfetrinem cilexetil

01 Mar 2023·Current Drug Research Reviews

Carbapenem Antibiotics: Recent Update on Synthesis and Pharmacological Activities

Review

Author: Verma, Navneet ; Tiwari, Abhishek ; Sahoo, Biswa Mohan ; Kumar, Manish ; Tiwari, Varsha ; Banik, Bimal Krishna

Abstract:Right from the breakthrough of carbapenems since 1976, many schemes on synthesis, structure-activity relationship (SAR), and biological activities have been carried out, and several carbapenems have been developed, including parentally active carbapenems like imipenem, doripenem, biapenem, meropenem, ertapenem, panipenem, razupenem, tomopenem, cilastatin, whereas orally active carbapenems like GV-118819, GV-104326, CS-834, L-084, DZ-2640, CL 191, 121, L-646, 591, S-4661, ER-35768, MK-826. Prodrugs of carbapenem with increased bioavailability include temopenem, tebipenem, sanfetrinem, LK-157, and CP 5484. Merck, Glaxo Welcome Research Group, Johnson & Johnson, Sankyo Group and Dai-ichi Group, and Wyeth-Ayerst Group were among the businesses that produced carbapenems. The Witting reaction, Mitsunobu reaction, Dieckmann reaction, palladium-catalyzed hydrogenolysis, E. coli-based cloned synthesis, and biosynthetic enzymes such as carbapenem synthetase (carA), carboxymethylproline synthase (carB), carbapenem synthase (carC). Carbapenems are biologically in infections like urinary tract infections, bloodstream infections, tuberculosis, intra-abdominal infections, and pathogens like anaerobes, gram-positive and gram-negative bacteria.

01 Jan 2000·MutagenesisQ3 · MEDICINE

Carboxylesterases, a key factor in evaluating potential genotoxicity of Trinem antibiotics

Q3 · MEDICINE

Article

Author: Vandin, L. ; Gatehouse, D. ; Pugnaghi, F. ; Naidoo, A. ; Oliver, J. ; Comelli, R.

Sanfetrinem cilexetil, a hexetil ester of a Trinem antibiotic, does not induce micronuclei in rat bone marrow cells or induce DNA repair synthesis in rat hepatocytes following oral dosing. However, in vitro chromosome damage and mutations are induced in mammalian cells lacking carboxylesterase activity (human lymphocytes and mouse lymphoma L5178Y cells). In cells possessing carboxylesterase activity (CHL cells), chromosome damage induced by Sanfetrinem cilexetil is not observed. Similarly, if induced rat liver preparations or non-induced preparations from rat or human intestinal cells are present during exposure, genotoxic activity is lost, even in those cells lacking carboxylesterase enzymes. Thus the lack of demonstrable genotoxicity in vivo, in the assays used, is likely to be due to hydrolysis of the parent molecule by non-specific carboxylesterases present within the intestinal epithelium. In turn this data indicates that a genotoxic hazard to humans under therapeutic conditions is unlikely.

01 Jul 1998·Antimicrobial Agents and ChemotherapyQ2 · MEDICINE

In Vivo Antibacterial Activities of Sanfetrinem Cilexetil, a New Oral Tricyclic Antibiotic

Q2 · MEDICINE

Article

Author: Ishii, Yoshikazu ; Furuya, Nobuhiko ; Tateda, Kazuhiro ; Matsumoto, Tetsuya ; Ohno, Akira ; Tamura, Shinobu ; Miyazaki, Shuichi ; Yamaguchi, Keizo

ABSTRACT The in vivo antibacterial activities of a new oral trinem, sanfetrinem cilexetil (a prodrug of sanfetrinem), were evaluated in comparison with those of cefdinir and amoxicillin. Sanfetrinem cilexetil showed potent efficacy against experimental murine septicemia caused by Staphylococcus aureus , Streptococcus pyogenes , and Escherichia coli and against murine respiratory infections caused by Streptococcus pneumoniae . Likewise, in murine models of respiratory infection by penicillin-susceptible and penicillin-resistant S. pneumoniae , sanfetrinem cilexetil was more effective than amoxicillin in reducing the number of bacteria in infected lungs. These results were reflected in its potent in vitro activity and high levels in plasma.

100 Deals associated with Sanfetrinem cilexetil

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