>> would be nice to
awaken this thread a little. :~) <<
Might be nice if you read the thread "a little" before you try awakening it. There is only one potential product nearing clinicals, the beta lactam. It is already partnered (Ortho). On 3/13/99 at an Informed Investors forum, Jim Rurka said that the mfg problems for MC-02,479 have been resolved. The first patient is likely to be treated by November at the latest (they've missed targets frequently, but I like this company and management team, and feel that they'll get on-track eventually).
The painful "pink if not red" flag..... a backup compound appears to be better.
Twenty chemists at Daichi and at MCDE working on the efflux pump inhibitors (levofloxacin complements). Had a preclinical candidate, but it didn't make it to development due to accumulation in tissues.
A journalist lurks in this thread. He is a particularly effective politician-ass who does not acknowledge his sources. I therefore will not go further. Disclaimer.... while I admire Rurka, Miller et al. and their efforts, I haven't owned MCDE in a long time.
(just parking the following here so that I can find it, if needed, in the future)........
Antimicrob Agents Chemother 1998 Nov;42(11):2956-60
Activities of new fluoroquinolones against fluoroquinolone-resistant
pathogens of the lower respiratory tract.
Piddock LJ, Johnson M, Ricci V, Hill SL
Antimicrobial Agents Research Group, Department of Infection, University of Birmingham, Birmingham, United Kingdom.
l.j.v.piddock@bham.ac.uk
The activities of six new fluoroquinolones (moxifloxacin, grepafloxacin, gatifloxacin, trovafloxacin, clinafloxacin, and
levofloxacin) compared with those of sparfloxacin and ciprofloxacin with or without reserpine (20 microg/ml) were determined
for 19 Streptococcus pneumoniae isolates, 5 Haemophilus sp. isolates, and 10 Pseudomonas aeruginosa isolates with
decreased susceptibility to ciprofloxacin from patients with clinically confirmed lower respiratory tract infections. Based upon
the MICs at which 50% of isolates were inhibited (MIC50s) and MIC90s, the most active agent was clinafloxacin, followed by
(in order of decreasing activity) trovafloxacin, moxifloxacin, gatifloxacin, sparfloxacin, and grepafloxacin. Except for
clinafloxacin (and gatifloxacin and trovafloxacin for H. influenzae), none of the new agents had improved activities compared
with that of ciprofloxacin for P. aeruginosa and H. influenzae. A variable reserpine effect was observed for ciprofloxacin and S.
pneumoniae; however, for 9 of 19 (47%) isolates the MIC of ciprofloxacin was decreased by at least fourfold, suggesting the
presence of an efflux pump contributing to the resistance phenotype. The laboratory parC (Ser79) mutant strain of S.
pneumoniae required eightfold more ciprofloxacin for inhibition than the wild-type strain, but there was no change in the MIC of
sparfloxacin and only a 1-dilution increase in the MICs of the other agents. For efflux pump mutant S. pneumoniae the activities
of all the newer agents, except for levofloxacin, were reduced. Except for clinafloxacin, all second-step laboratory mutants
required at least 2 microg of all fluoroquinolones per ml for inhibition. |
