Pamicogrel is a cyclooxygenase inhibitor with platelet anti-aggregatory properties which is under development by Kanebo for chronic arterial occlusion. It also has potential in both prophylaxis and treatment of ischemic brain injury. An NDA was submitted in Japan in April 1997. The effects of the drug on platelet aggregation were originally disclosed in EP-00159677, while the later European patent, EP-00560136, claims its use in brain dysfunction induced by hypoxia arising from disturbance of cerebral circulation, such as cerebral hemorrhage or cerebral infarction.

01 Sep 1997·European Journal of PharmacologyQ3 · MEDICINE

Antithrombotic effects in a rat model of aspirin-insensitive arterial thrombosis of desethyl KBT-3022, the main active metabolite of a new antiplatelet agent, KBT-3022

Q3 · MEDICINE

Article

Author: Masamitsu Shimazawa ; Kazunao Kondo ; Mitsuyoshi Nakashima ; Kazuo Umemura ; Yoshiharu Takiguchi

The antithrombotic effect of desethyl KBT-3022, which is the main active metabolite of the new antiplatelet agent, KBT-3022 (ethyl 2-[4,5-bis(4-methoxyphenyl)thiazol-2-yl] pyrrol-1-ylacetate; a cyclooxygenase inhibitor), was determined using a photochemically induced arterial thrombosis model in the rat femoral artery. Pretreatment with desethyl KBT-3022 (0.1, 0.3 and 1 mg/kg, i.v.) prolonged the time required to achieve thrombotic occlusion in the femoral artery and inhibited collagen-induced platelet aggregation in whole blood ex vivo, each in a dose-dependent manner. In all 6 rats used, particularly at the highest dose (1 mg/kg, i.v.) tested, cyclic variations in blood flow were hardly ever observed and complete cessation of blood flow did not occur during the 30-min observation time. BM-13505 (1, 3 and 10 mg/kg, i.v.), a thromboxane A2 receptor antagonist, also prolonged the time to occlusion, but cyclic variations in blood flow did occur. On the other hand, aspirin (10 and 30 mg/kg, i.v.) had little effect in terms of preventing thrombosis, although it inhibited collagen-induced platelet aggregation to the same extent as did desethyl KBT-3022. Desethyl KBT-3022 inhibited the thrombin-induced aggregation of washed platelets in a concentration-dependent manner (1-40 microM), whereas aspirin and BM-13505 did not. These findings suggest that the potent antithrombotic effect of desethyl KBT-3022 may be attributable in part to its additional ability to inhibit thrombin-induced platelet aggregation. Accordingly, thromboxane A2 and thrombin may be important thrombotic mediators in this rat model.

01 Feb 1997·General Pharmacology: The Vascular System

The mechanism of action of KBT-3022, a new antiplatelet agent

Article

Author: Konomi Matsuo ; Koichi Yokota ; Akira Yamashita ; Minoru Oda

1. The mechanism of action of a new antiplatelet agent, KBT-3022 (ethyl 2-[4,5-bis(4-methoxyphenyl)thiazol-2-yl]pyrrol-1-ylacetate) and its active main metabolite, desethyl KBT-3022, was investigated. 2. KBT-3022 and desethyl KBT-3022 inhibited cyclooxygenase from ovine seminal gland with IC50 values of 0.69 and 0.43 microM, respectively. 3. At concentrations higher than those required for cyclooxygenase inhibition, desethyl KBT-3022 inhibited cAMP-phosphodiesterase, specific binding of U46619, and release of phosphatidic acid from thrombin-stimulated platelets. 4. Oral administration of KBT-3022 inhibited the production of thromboxane B2 during blood coagulation more potently than the production of 6-keto-prostaglandin F1 alpha from aortic strips in guinea pigs. 5. These findings suggest that KBT-3022 may inhibit platelet activation principally via the inhibition of cyclooxygenase by desethyl KBT-3022.

100 Deals associated with Pamicogrel

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KEGG	Wiki	ATC	Drug Bank
D01090	Pamicogrel	-	-

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Indication	Highest Phase	Country/Location	Organization	Date
Arterial Occlusive Diseases	NDA/BLA	-	Akzo Nobel NV	-
Arterial Occlusive Diseases	NDA/BLA	JP	-	-
Arterial Occlusive Diseases	NDA/BLA	-	Torii Pharmaceutical Co., Ltd.	-

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