scholarly journals In Vitro Activity of Mirincamycin (U24729A) against Plasmodium falciparum Isolates from Gabon

2009 ◽  
Vol 54 (1) ◽  
pp. 540-542 ◽  
Author(s):  
Jana Held ◽  
Richard Westerman ◽  
Peter G. Kremsner ◽  
Benjamin Mordmüller

ABSTRACT We assessed the in vitro activity of mirincamycin, a lincosamide antibiotic, against Plasmodium falciparum clinical isolates from Gabon. Growth was determined by HRP2 enzyme-linked immunosorbent assay using an adapted protocol with a prolonged incubation time (6 days) to account for antibiotic-induced delayed death. Mirincamycin's cis and trans isomers are more active (median 50% inhibitory concentrations [IC50s], 3.2 nM and 2.6 nM) than the comparator drugs clindamycin (IC50, 12 nM) and doxycycline (IC50, 720 nM), and therefore, further clinical development is promising.

1998 ◽  
Vol 42 (9) ◽  
pp. 2347-2351 ◽  
Author(s):  
Leonardo K. Basco ◽  
Jean Bickii ◽  
Pascal Ringwald

ABSTRACT The in vitro antimalarial activity of the new Chinese synthetic drug, lumefantrine, also known as benflumetol (a fluorene derivative belonging to the aminoalcohol class), was determined by an isotopic microtest against 61 fresh clinical isolates of Plasmodium falciparum and compared with that of other established antimalarial agents. The geometric mean 50% inhibitory concentration of lumefantrine was 11.9 nmol/liter (95% confidence intervals, 10.4 to 13.6 nmol/liter; range, 3.3 to 25.6 nmol/liter). The in vitro activities of lumefantrine against the chloroquine-sensitive and the chloroquine-resistant isolates did not differ (P > 0.05). There was a significant positive correlation of responses between lumefantrine and two other aminoalcohols studied, mefloquine (r = 0.688) and halofantrine (r = 0.677), and between lumefantrine and artesunate (r = 0.420), suggesting a potential for in vitro cross-resistance. Our data suggest high in vitro activity of lumefantrine, comparable to that of mefloquine, and are in agreement with the promising results of preliminary clinical trials.


2010 ◽  
Vol 35 (6) ◽  
pp. 587-589 ◽  
Author(s):  
Jana Held ◽  
Philipp Zanger ◽  
Saadou Issifou ◽  
Peter G. Kremsner ◽  
Benjamin Mordmüller

2019 ◽  
Vol 63 (9) ◽  
Author(s):  
Amit Kaushik ◽  
Nicole C. Ammerman ◽  
Nicole M. Parrish ◽  
Eric L. Nuermberger

ABSTRACT The new diazabicyclooctane-based β-lactamase inhibitors avibactam and relebactam improve the in vitro activity of β-lactam antibiotics against bacteria of the Mycobacterium abscessus complex (MABC). Here, we evaluated the in vitro activities of two newer diazabicyclooctane-based β-lactamase inhibitors in clinical development, nacubactam and zidebactam, with β-lactams against clinical isolates of MABC. Both inhibitors lowered the MICs of their partner β-lactams, meropenem (8-fold) and cefepime (2-fold), respectively, and those of other β-lactams, similar to prior results with avibactam and relebactam.


2019 ◽  
Author(s):  
Amit Kaushik ◽  
Nicole C. Ammerman ◽  
Nicole M. Parrish ◽  
Eric L. Nuermberger

AbstractThe new diazabicyclooctane-based β-lactamase inhibitors avibactam and relebactam improve the in vitro activity of β-lactam antibiotics against Mycobacterium abscessus complex (MABC). Here, we evaluated the in vitro activity of two newer diazabicyclooctane-based β-lactamase inhibitors in clinical development, nacubactam and zidebactam, with β-lactams against clinical isolates of MABC. Both inhibitors lowered the MICs of their partner β-lactams, meropenem (eight-fold) and cefepime (two-fold), and those of other β-lactams, similar to prior results with avibactam and relebactam.


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