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Dosage regimen for prasugrel

A technology of prasugrel hydrochloride and medicinal salts, which can be used in medical formulas, drug combinations, extracellular fluid diseases, etc., can solve plaque rupture and other problems, and achieve the effect of preventing the occurrence or recurrence of vascular diseases

Inactive Publication Date: 2008-06-11
ELI LILLY & CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the processes that cause vascular disease are complex and not fully understood, the basic etiology shared by many theories includes atherosclerosis due to the formation of atherosclerotic lesions and plaque rupture leading to thrombosis or thromboembolism

Method used

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  • Dosage regimen for prasugrel
  • Dosage regimen for prasugrel
  • Dosage regimen for prasugrel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055]Mix prasugrel HCl (10.98 mg / tablet, equivalent to 10 mg base / tablet), mannitol, hydroxypropyl methylcellulose, croscarmellose sodium, microcrystalline cellulose and magnesium stearate, The granulation is then roller compacted. To the resulting granulate was added further croscarmellose sodium, microcrystalline cellulose and magnesium stearate, the materials were mixed and compressed into tablets weighing 250 mg. The Opadry(R) II beige film coating mixture was added to the water and sprayed onto the tablets in a side vented coating pan.

[0056] Clinical Example 1

[0057] A comparative study of the effects of prasugrel and clopidogrel on platelet function in healthy subjects

[0058] Background: Antiplatelet agents such as aspirin and clopidogrel are effective in the secondary prevention of atherosclerotic events. In preclinical studies, prasugrel showed more potent inhibition of platelet aggregation (IPA) than clopidogrel. This study examined the tolerability, safet...

Embodiment 2

[0065] In aspirin-treated patients with atherosclerotic vascular disease, prasugrel achieved significantly higher inhibition of platelet aggregation and a lower rate of non-responders compared with clopidogrel.

[0066] Background: Lower levels of inhibition of platelet aggregation (IPA) with clopidogrel increase the risk of thrombotic events. This study analyzed the use of novel P2Y compared with clopidogrel (Clop) in aspirin-treated patients. 12 IPA and non-responder rates for the antagonist prasugrel (Pras).

[0067] METHODS: After 7 days of aspirin 325 mg, 101 subjects were randomly assigned to one of five regimens, with a loading dose (LD) on day 1 and a daily maintenance dose (MD) on days 2-28. ): Prasugrel - 40 mg LD / 5 mg MD, 40 mg LD / 7.5 mg MD, 60 mg LD / 10 mg MD or 60 mg LD / 15 mg MD, or clopidogrel - 300 mg LD / 75 mg MD. IPA to 20 μM ADP was measured by turbidometric aggregometry. Non-responders were defined as those subjects who did not achieve > 20% IPA at pre-dose...

Embodiment 3

[0074] Clopidogrel responders and non-responders: with the new thienopyridine P2Y 12 Receptor antagonist prasugrel vs.

[0075] Background: Lower levels of inhibition of platelet aggregation (IPA) with clopidogrel have been associated with a higher risk of adverse events after percutaneous coronary intervention (PCI). Identification of clopidogrel and novel thienopyridine P2Y using objectively defined IPA thresholds according to Bayesian classification theory 12 Responders and non-responders to the receptor antagonist prasugrel.

[0076] METHODS: A comprehensive database of ADP (5 μM and 20 μM)-induced platelet aggregation measured by nephelometric aggregometry from three single-center crossover clinical pharmacology studies was analyzed. Subjects (N=112, aged 18-65 years old) were healthy volunteers whose baseline maximum platelet aggregation (MPA)>70% to 20μM ADP, these subjects were randomly divided into clopidogrel 300mg loading dose ( LD) or prasugrel 60mg LD. The cha...

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Abstract

Abstract A dosage regimen for treating vascular disease in a human comprising the steps of administering a loading dosage of about 30 mg to 70 mg of loading dose of prasugrel or a pharmaceutically acceptable salt thereof, and thereafter administering a daily dosage regimen of about 7.5 mg to 15 mg maintenance dose of prasugrel or a pharmaceutically acceptable salt thereof.

Description

field of invention [0001] The present invention relates to dosing regimens for administering prasugrel to a patient in need thereof. Background of the invention [0002] Vascular disease, including myocardial infarction and ischemic stroke, is a leading cause of death and disability. Although the processes leading to vascular disease are complex and not fully understood, the basic etiology shared by many theories includes atherosclerosis due to the formation of atherosclerotic lesions and plaque rupture leading to thrombosis or thromboembolism. [0003] 2-Acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine (prasugrel)—— An adenosine diphosphate (ADP) receptor antagonist - a potent inhibitor of ADP-mediated platelet aggregation in vivo. US Patent 5,288,726 discloses tetrahydrothienopyridine derivatives including prasugrel. US Patent 6,693,115 B2 discloses acid addition salts of prasugrel. US Patent Publication 2004 / 0024013 Al discloses...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/47
CPCA61K31/4365A61P43/00A61P7/02A61P9/00A61P9/10A61K31/4743
Inventor J·T·勃兰特N·A·法里德J·A·雅库博夫斯基C·D·佩恩G·J·维拉科迪K·J·温特斯
Owner ELI LILLY & CO
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