RBx 7,796: A novel inhibitor of 5-lipoxygenase.

RBx 7,796: A novel inhibitor of 5-lipoxygenase. Research Abstract Details 

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RBx 7,796: A novel inhibitor of 5-lipoxygenase. Abstract Text:

R K Shirumalla,K S Naruganahalli,S G Dastidar,V Sattigeri,G Kaur,C Deb,J B Gupta,M Salman,A Ray,

OBJECTIVE: To evaluate the pharmacological profile of RBx 7,796, a novel 5-lipoxygenase inhibitor. MATERIALS AND METHODS: RBx 7,796 was evaluated for 5- lipoxygenase inhibitory potential using human recombinant enzyme and profiled for selectivity against 12 and 15 lipoxygenase. RBx 7,796 was evaluated in cell based assay for inhibition of A23,187 induced LTB(4) release from isolated neutrophils. Ex vivo activity was evaluated for inhibition of A23,187 induced LTB(4) release in blood from treated rats. In vivo efficacy of RBx 7,796 was profiled in LPS induced neutrophilia model in rats and also in ovalbumin induced bronchoconstriction and airway inflammation models in guinea pigs. RESULTS: RBx 7,796, a novel chemotype, showed competitive inhibition of 5-lipoxygenase enzyme with an IC(50) of 3.5 +/- 1.1 microM. RBx 7,796 offered >100 fold selectivity against other related enzymes - 12 and 15 lipoxygenase. RBx 7,796 inhibited release of LTB(4) from human and rat neutrophils in vitro. Upon administration to rats, RBx 7,796 inhibited A23,187 induced LTB(4) release from rat neutrophils. Upon repeated administration, dosed once daily, RBx 7,796 inhibited LPS induced neutrophil influx in rat airway. RBx 7,796 also inhibited allergen induced bronchoconstriction and eosinophil influx in guinea pig airway in a dose dependent manner. CONCLUSION: The results suggest that RBx 7,796, a novel chemotype, is an orally efficacious inhibitor of 5-lipoxygenase enzyme that is effective against both neutrophilic and eosinophilic airway inflammation and shows potent inhibition with once daily administration.

RBx 7,796: A novel inhibitor of 5-lipoxygenase. Publishing Authors By Initials

RK Shirumalla,KS Naruganahalli,SG Dastidar,V Sattigeri,G Kaur,C Deb,JB Gupta,M Salman,A Ray,

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RBx 7,796: A novel inhibitor of 5-lipoxygenase. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Inflammation research : official journal of the Eu

VOLUME: 55

Page Numbers: 517-27

Journal Abbreviation: Inflamm. Res.

ISSN: 1023-3830

DAY: 15

MONTH: Dec

YEAR: 2006

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LANGUAGE: eng

NlmUniqueID: 9508160

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AFFILIATION: Department of Pharmacology, New Drug Discovery Research, Ranbaxy Research Laboratories, Plot No-20, Sector-18, Udyog Vihar, Gurgaon, Haryana 122015, India.

Country: Switzerland

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MEDLINETA: Inflamm Res

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