Biapenem is a broad-spectrum carbapenem antibiotic with activity against Gram-positive and Gram-negative bacteria. It is useful for pathogens causing intra-abdominal, lower respiratory, and urinary tract infections. It is highly resistant to most types of β-lactamases from both aerobes and anaerobes. It is a 1-β-methylcarbapenem and has similar antibacterial activity to Imipenem, with less neurotoxicity and increased stability against human renal dehydropeptidase-I. The compound can be used in pharmacokinetic studies.
Biapenem is sparingly soluble in water.
| Mechanism of Action | Biapanem has a similar structure and activity to imipenem but has a methyl group in the 1-beta position. Addition of the methyl group confers resistance to human renal dehydropeptidase-I (DHP-1). |
| Spectrum | Biapanem, similar to Imipenem, has activity against Gram-positive and Gram-negative bacteria, both aerobic and anaerobic. |
| Microbiology Applications | The in vitro and in vivo activity of Biapenem was compared to imipenem, meropenem and others, against 441 anaerobes. It had activity comparable to imipenem and meropenem against all groups of anaerobes with MICs for 90% strains tested of 0.06 to 2 µg/ml and 98.6% of strains at ≤ 1 µg/ml, indicating excellent performance against anaerobic bacteria. It is active against B. capillosus, Prevotella, Clostridum, and Eubacterium strains. Exceptions include type I, chromosomally mediated β-lactamases from aerobic, Gram-negative bacilli, and the metallo-containing β-lactamases of anaerobes. (Tsuji et al, 1998). To review additional MICs for Biapenem from the Antimicrobial Database, click here. |
| Molecular Formula | C15H18N4O4S |
| References |
Aldridge KE, Morice N and Schiro DD (1994) In vitro activity of biapenem (L-627), a new carbapenem, against anaerobes. Antimicrob. Agents Chemother. 38(4):889-93 PMID 8031067 Malanoski GJ, Collins L, Wennersten C, Moellering RC, and Eliopoulos GM (1993) In vitro activity of biapenem against clinical isolates of Gram-positive and Gram-negative bacteria. Antimicrob. Agents Chemother. 37(9):2009-2016 Masakatsu Tsuji, Yoshikazu Ishii, Akira Ohno, Shuichi Miyazaki, and Keizo Yamaguchi 1998. In vitro and in vivo antibacterial activities of S-4661, a new carbapenem antimicrobial agents and chemotherapy Vol. 42, No. 1, p. 94–99 PMID 9449267 Perry CM and Ibbotson T (2002) Biapenem. Drugs 62(15):2221-2234 PMID 12381221 Singh BK and Macdonald CA (2010) Drug discovery from uncultivable microorganisms. Drug Disc. Today 15(17):792-799 |