Reference

Antigenicity of the new quinolone antibacterial agent levofloxacin

Antigenicity of the new quinolone antibacterial agent levofloxacin. Wagai, N.; Hattori, H.; Yamaguchi, F.; Takayama, S. (Drug Saf. Res. Cent., Daiichi Pharm. Co., Ltd., Tokyo, Japan). Arzneim.-Forsch., 42(3A), 385-9 (English) 1992. CODEN: ARZNAD. ISSN: 0004-4172. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) An antigenicity study of a new quinolone antibacterial agent, lefovloxacin (DR-3355, CAS 100986-85-4), was carried out in mice, guinea pigs and rabbits with passive cutaneous anaphylaxis (PCA), systemic anaphylaxis (SA) and enzyme linked immunosorbent assay (ELISA). Mice were sensitized with DR-3355 (1-100 mg/kg) or DR-3355-ovalbumin (OA) conjugate (DR-3355-OA; 500 mg/kg). No IgE antibodies to DR-3355 were detected in the sera obtained from the DR-3355-sensitized mice, indicating that DR-3355 has no immunogenicity in mice. By using DR-3355-OA has a sensitizing antigen, DR-3355-specific IgE was produced successfully in 7 out of 10 sera, and 4 sera showed pos. responses in 24-h PCA on i.v. injection of DR-3355 (40 mg/kg). These responses disappeared on challenge with a dose of 2.5 mg/kg. Guinea pigs or rabbits were sensitized with DR-3355 (2-100 or 2-20 mg/kg) or DR-3355-OA (2 mg/kg). No SA was obsd. in the sensitized guinea pigs after the i.v. injection of DR-3355 (40 mg/kg). No antibodies to DR-3355 were detected in the sera obtained from the sensitized guinea pigs and rabbits by PCA or ELISA. These results suggest that DR-3355 may not possess antigenicity in guinea pigs and rabbits. On the other hand, the results of PCA in mice suggest that DR-3355 may have eliciting antigenicity potential.

Mutagenicity of the new quinolone antibacterial agent levofloxacin

Mutagenicity of the new quinolone antibacterial agent levofloxacin. Shimada, H.; Itoh, S.; Hattori, C.; Tada, S.; Matsuura, Y. (Drug Saf. Res. Cent., Daiichi Pharm. Co., Ltd., Tokyo, Japan). Arzneim.-Forsch., 42(3A), 378-85 (English) 1992. CODEN: ARZNAD. ISSN: 0004-4172. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) A new quinolone antibacterial agent levofloxacin (DR-3355, CAS 100986-85-4), was studied for mutagenicity using the following short-term in vitro and in vivo tests. 1 In vitro studies: reverse mutation test (Ames method) on S. typhimurium and E. coli; and HGPRT forward mutation test, cytogenetic test, and sister chromatid exchange (SCE) test, all on Chinese hamster cells. 2 In vivo studies: mouse micronucleus test, SCE test on mouse bone marrow cell, in vivo-in vitro unscheduled DNA synthesis (UDS) test on rat primary hepatocytes, and dominant lethal test in BDG1 mice. In the in vitro tests for SCE and for chromosomal aberration, DR-3355 gave dose-dependent pos. responses, but no mutagenicity was obsd. in the same indicators of the in vivo studies, even at the max. tolerated doses. This strongly suggested that DR-3355 would have no mutagenic effects when used in the treatment of infectious diseases. DR-3355 did not show any pos. response in the reverse mutation test, the HGPRT mutation test, the in vivo-in vitro UDS test or the dominant lethal test.