Peptide deformylase (PDF) is a class of metalloenzyme responsible for catalyzing the removal of the N-formyl group from N-terminal methionine following translation. PDF inhibitors are moving into new phase of drug development. Initially, PDF was considered as an important target in antibacterial drug discovery; however genome database searches have revealed PDF-like sequences in parasites (P. falciparum) and human, widening the utility of this target in antimalarial and anticancer drug discovery along with antibacterial. Using structural and mechanistic information together with high throughput screening, several types of chemical classes of PDF inhibitors with improved efficacy and specificity have been identified. Various drugs like, GSK-1322322 (Phase II), BB-83698 (Phase I), and LBM-415 (Phase I) have entered into clinical developments. Developments in the field have prompted us to review the current aspects of PDFs, especially their structures, different classes of PDF inhibitors, and molecular modeling studies. In nut shell, this review enlightens PDF as a versatile target along with its inhibitors and future perspectives of different PDF inhibitors.

01 Aug 2011·Clinical Pharmacology & TherapeuticsQ2 · MEDICINE

Pharmacokinetics and Unexpected Safety Issues of LBM415, a Novel Oral Peptide Deformylase Inhibitor

Q2 · MEDICINE

Article

Author: H Sun ; TG Evans ; P Rolan ; C MacLeod ; K Bracken

Peptide deformylase (PDF) inhibitors represent a potential new class of antibiotics targeting a large number of bacterial species. We studied the pharmacokinetics and safety of LBM415, a novel PDF inhibitor, administered as a single oral dose at 100-3,000 mg in the fasted state and at 1,000 mg in the fed state in healthy volunteers. LBM415 was then administered at dosages ranging from 100 mg q.d. to 1,000 mg t.i.d. for 11 days. Dose-proportional pharmacokinetics was observed, with a peak plasma concentration (C(max)) of 17.85 ± 5.96 µg/ml at 1,000 mg b.i.d. (the projected therapeutic dose) and an area under the concentration-time curve (AUC)(0-24h) of 36.83 ± 10.36 µg/ml·h. The half-life, as determined after a 1,000-mg single dose, was 2.18 ± 0.61 h. The compound was well tolerated at low doses, but at the highest dose, 1,000 mg t.i.d., reversible cyanosis and low oxygen saturation, attributable to methemoglobinemia, were detected on day 11. Oxygen saturation was as low as 88% in one subject on day 11.

01 Mar 2011·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

Synthesis and in vitro antibacterial activity of oxazolidine LBM-415 analogs as peptide deformylase inhibitors

Q4 · MEDICINE

Article

Author: Weicheng Zhou ; Zhenyu Wang ; Linliang Yu

The drug resistant bacteria pose a severe threat to human health. The increasing resistance of those pathogens to traditional antibacterial therapy renders the identification of new antibacterial agents with novel antibacterial mechanisms an urgent need. In this study, a series of (2S)-N-substituted-1-[(formyhydroxyamino)methyl]-1-oxohexyl]-2-oxazolidinecarboxamides were designed, synthesized and evaluated for in vitro antibacterial activity. Most of these compounds displayed good activities against Gram-positive organisms comparable to reference agent LBM-415.

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Indication	Highest Phase	Country/Location	Organization	Date
Bacterial Infections	Phase 2	-	Novartis Pharma AG	-
Bacterial Infections	Phase 2	-	Pfizer Inc.	-
Pneumonia	Phase 2	-	Pfizer Inc.	-
Pneumonia	Phase 2	-	Novartis Pharma AG	-
Gram-Negative Bacterial Infections	Preclinical	US	Vicuron Pharmaceuticals LLC	05 Jun 2002
Gram-Positive Bacterial Infections	Preclinical	US	Vicuron Pharmaceuticals LLC	05 Jun 2002

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