PPARγ agonists(Peroxisome proliferator-activated receptor γ agonists), SGLT2 inhibitors(Sodium/glucose cotransporter 2 inhibitors), Insulin sensitizers

Therapeutic Areas

Immune System DiseasesEndocrinology and Metabolic DiseaseSkin and Musculoskeletal Diseases

Active Indication-

Inactive Indication

Diabetes Mellitus, Type 2Rheumatoid Arthritis

Originator Organization

Theracos, Inc.

Active Organization-

Inactive Organization

Theracos, Inc.Bailu Pharmaceutical Technology(Shanghai)Co.,Ltd.

Drug Highest PhasePendingIND Application

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC28H25NO7S

InChIKeyIVAQJHSXBVHUQT-UHFFFAOYSA-N

CAS Registry249886-47-3

100 Clinical Results associated with CLX-0921

100 Translational Medicine associated with CLX-0921

100 Patents (Medical) associated with CLX-0921

Literatures (Medical) associated with CLX-0921

01 Apr 2004·Journal of Molecular EndocrinologyQ3 · MEDICINE

Cinnamic acid based thiazolidinediones inhibit human P450c17 and 3beta-hydroxysteroid dehydrogenase and improve insulin sensitivity independent of PPARgamma agonist activity

Q3 · MEDICINE

Article

Author: Gross, Coleman ; Miller, Walter L. ; Arlt, Weibke ; Neogi, Partha

Thiazolidinediones improve insulin sensitivity in type 2 diabetes mellitus by acting as peroxisome proliferator-associated receptor gamma (PPARgamma) agonists, and decrease circulating androgen concentrations in polycystic ovary syndrome by unknown mechanisms. Some thiazolidinediones directly inhibit the steroidogenic enzymes P450c17 and 3beta-hydroxysteroid dehydrogenase type II (3betaHSDII) by distinct mechanisms. We synthesized five novel thiazolidinediones, CLX-M1 to -M5 by linking a 2,4-thiazolidinedione moiety to a substituted alpha-phenyl cinnamic acid previously shown to have glucose-lowering effects. Using yeast microsomes expressing human P450c17 and 3betaHSDII we found that cinnamic acid methyl esters with a double bond in the thiazolidinedione core structure (M3, M5) were stronger inhibitors of P450c17 than methyl esters with the conventional core (M1, M4). These four compounds inhibited 3betaHSDII equally well, while the free cinnamic acid analog (M2) did not inhibit either enzyme. Thus, the inhibition of P450c17 and 3betaHSDII by these novel thiazolidinediones reveals structure-activity relationships independent of PPARgamma transactivation. PPARgamma transactivation was moderate (M1), weak (M2, M3) or even absent (M4, M5). While the PPARgamma agonist activity of M1 was only 3% of that of rosiglitazone, both increased glucose uptake by 3T3-L1 adipocytes and reduced serum glucose levels in ob/ob and db/db mice to a similar extent. The similar glucose-lowering effects of M1 and rosiglitazone, despite their vast differences in PPARgamma agonist activity, suggests these two actions may occur by separate mechanisms.

01 Aug 2003·MetabolismQ1 · MEDICINE

A novel peroxisome proliferator-activated gamma (PPARγ) agonist, CLX-0921, has potent antihyperglycemic activity with low adipogenic potential

Q1 · MEDICINE

Article

Author: Somesh D Sharma ; Coleman Gross ; Gerald M Reaven ; Debendranath Dey ; Partha Neogi ; Maya Gowri ; Jin Cheng ; Satya Medicherla ; Bishwajit Nag

Agonists of the nuclear receptor peroxisome proliferator-activated receptor gamma (PPAR gamma) are pharmacologically active antihyperglycemic agents that act by increasing peripheral tissue sensitivity to insulin. Many of these agonists have antihyperglycemic activity that is directly proportional to their ability to bind and activate PPAR gamma; however, recent data bring this relationship into question. In this report we describe a new PPAR gamma agonist, CLX-0921, that is derived from a natural product. This thiazolidinedione (TZD) has a spectrum of activity that differs from commercially available TZDs. It is a weak activator of PPAR gamma (EC(50) of 0.284 micromol/L) compared to rosiglitazone (EC(50) 0.009 micromol/L). Despite this difference, the drug maintains potent glucose uptake activity in vitro and glucose-lowering activity in vivo that is equipotent to that of rosiglitazone. Moreover, CLX-0921 showed a 10-fold reduction in in vitro adipogenic potential compared to rosiglitazone. CLX-0921 also increases glycogen synthesis, an activity not typically associated with rosiglitazone or pioglitazone. Thus CLX-0921 appears to have a distinct spectrum of activity relative to other TZDs.

01 May 2001·Current opinion in investigational drugs (London, England : 2000)

CLX-0901 (Calyx Therapeutics).

Review

Author: Barlocco, D

Calyx Therapeutics is developing the insulin sensitizer, CLX-0901, as an antidiabetic agent. CLX-0901 is the synthetic analog of CLX-0900 which was originally isolated from a plant source. Phase I and toxicological studies indicate that the compound is safe and well tolerated [363764]. As of March 2001, phase II studies had commenced [402737]. Other antidiabetics being investigated by Calyx include CLX-0301, CLX-0921, CLX-0940, CLX-0100 and CLX-0101 [376032].

100 Deals associated with CLX-0921

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB05854

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	IND Application	China	Theracos, Inc.	28 Mar 2005
Diabetes Mellitus, Type 2	IND Application	China	Bailu Pharmaceutical Technology(Shanghai)Co.,Ltd.	28 Mar 2005
Rheumatoid Arthritis	IND Application	China	Bailu Pharmaceutical Technology(Shanghai)Co.,Ltd.	28 Mar 2005
Rheumatoid Arthritis	IND Application	China	Theracos, Inc.	28 Mar 2005

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