5-LOX inhibitors(Arachidonate 5-lipoxygenase inhibitors), PLA2 inhibitors(Phospholipases A2 inhibitors), PLA2G2A inhibitors(Phospholipase A2 group IIA inhibitors)

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Therapeutic Areas

Skin and Musculoskeletal Diseases

Active Indication

Arthritis

Inactive Indication

Inflammationischemic brain injury

Originator Organization

Eli Lilly & Co.

Active Organization

Lilly Research Laboratories

Inactive Organization

Eli Lilly & Co.

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure

Molecular FormulaC18H25NO2S

InChIKeyBUDGLLLMROWLOB-UHFFFAOYSA-N

CAS Registry107889-32-7

100 Clinical Results associated with LY-178002

100 Translational Medicine associated with LY-178002

100 Patents (Medical) associated with LY-178002

Literatures (Medical) associated with LY-178002

01 Jun 1994·Annals of the New York Academy of SciencesQ2 · CROSS-FIELD

Novel Antioxidant Therapy for Cerebral Ischemia‐Reperfusion Injury

Q2 · CROSS-FIELD

Article

Author: Jill Ann Panetta ; James A. Clemens

Antioxidants, LY178002 and LY231617, were as therapeutic agents i.m.=n models of both global and focal cerebral ischemia.

01 Aug 1991·StrokeQ1 · MEDICINE

LY178002 reduces rat brain damage after transient global forebrain ischemia.

Q1 · MEDICINE

Article

Author: Clemens, J A ; Ho, P P ; Panetta, J A

Several feasible mechanisms have been proposed as sources of neuronal damage from ischemia and subsequent reperfusion. Included among these are oxidative damage caused by free radical production and lipid peroxidation and products derived from phospholipid breakdown. A series of 4-thiazolidinone compounds represented by LY178002 (5-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]methylene-4-thiazolidinon e) have been described as inhibitors of multiple enzymes in the arachidonic acid cascade, including fatty acid cyclooxygenase, 5-lipoxygenase, and phospholipase A2. Accordingly, we evaluated LY178002 in a four-vessel occlusion model of global forebrain ischemia with reperfusion. A 2-hour pretreatment of 11 male Wistar rats with 150 mg/kg LY178002 significantly protected against striatal (p = 0.0007) and hippocampal CA1 (p = 0.006) damage after 30 minutes of global ischemia. Similar protection was observed for the striatum (p = 0.005) and hippocampal CA1 layer (p = 0.025) after pretreatment of 13 rats with 50 mg/kg LY178002. We further evaluated LY178002 as a possible inhibitor of lipid peroxidation because part of its chemical structure incorporates the aromatic backbone of the known antioxidant butylated hydroxytoluene. We found LY178002 to be a potent inhibitor of iron-dependent lipid peroxidation. Few substances possessing a single pharmacological activity have been found to be of significant therapeutic benefit in global ischemia of 30 minutes' duration because the mechanisms that lead to cell death in response to ischemia are likely to be multifactorial. Thus, the efficacy of LY178002 in this model may be due to its ability to inhibit multiple sources of damage.

01 Jun 1989·Agents and Actions

The anti-inflammatory effects of LY178002 and LY256548

Article

Author: P. P. K. Ho ; L. Wang ; R. D. Towner ; M. L. Phillips ; J. A. Panetta ; B. Bertsch ; D. N. Benslay

LY178002 (5-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]methylene-4-thiazolidinon e) and its N-methyl analog, LY256548, inhibit the enzymatic activity of phospholipase A2, 5-lipoxygenase and fatty acid cycloxygenase. They also inhibit leukotriene B4 production from human polymorphonuclear leukocytes stimulated with the calcium ionophore A23187. Since products of the arachidonic acid cascade have been implicated as important mediators in a variety of inflammatory diseases including arthritis, LY178002 and LY256548 were studied in the Freund's Complete Adjuvant-Induced Arthritis (FCA) model in rats. The compounds were administered orally and inhibition of bone damage and paw swelling was assessed of both the injected and uninjected paws. At 50 mg/kg LY178002 inhibited soft tissue swelling in the uninjected paw by 81% while LY256548 exhibited 57% inhibition. Bone damage was also significantly inhibited by both compounds. A dose response was conducted. The minimum effective dose for LY178002 was 10 mg/kg p.o. In the established FCA model LY178002 at 50 mg/kg p.o. inhibited the uninjected paw swelling by 75% while LY256548 did not show this level of activity. These results suggest that LY178002 and LY256548 may be useful in the treatment of arthritis.

100 Deals associated with LY-178002

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Arthritis	Preclinical	US	Lilly Research Laboratories	01 Jun 1989
Inflammation	Preclinical	US	Eli Lilly & Co.	08 Aug 1986
ischemic brain injury	Preclinical	US	Eli Lilly & Co.	08 Aug 1986

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