How to Handle Drug Polymorphs… Case Study of Trelagliptin Succinate

New Drug Approvals

Pharmaceutical API Polymorphs… case study of Trelagliptin
CASE STUDY WITH..Compound I having the formula
Figure imgf000073_0001
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WO2008067465A1 OR US8084605  IS THE PATENT USED AND WITH FORM “A” AND AMORPHOUS FORM
Active pharmaceutical ingredients (APIs), frequently delivered to the patient in the solid-state as part of an approved dosage form, can exist in such diverse solid forms as polymorphs, pseudopolymorphs, salts, co-crystals and amorphous solids. Various solid forms often display different mechanical, thermal, physical and chemical properties that can remarkably influence the bioavailability, hygroscopicity, stability and other performance characteristics of the drug.
Hence, a thorough understanding of the relationship between the particular solid form of an active pharmaceutical ingredient (API) and its functional properties is important in selecting the most suitable form of the API for development into a drug product. In past decades, there have been significant efforts on the discovery, selection and control…

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Idrabiotaparinux for anticoagulant therapy.

New Drug Approvals

Figure imgf000003_0002

Idrabiotaparinux

  •  抗血栓治療中の出血率を低下させるためのイドラビオタパリナックスの使用

(biotinylated idraparinux, SSR-126517, SSR-126517E)

405159-59-3              9 x Na salt
774531-07-6 (free acid)

Idrabiotaparinux has an attached biotin moiety at the non-reducing end unit, which allows its neutralisation with avidin, an egg-derived protein with low antigenicity. This compound is currently investigated in clinical trials for prevention of recurrent VTE in patients with acute pulmonary embolism. The future of idrabiotaparinux depends also on the safety and efficacy of avidin.
Symptomatic deep vein thrombosis (DVT) and/or pulmonary embolism (PE) – treatment and secondary prevention of recurrent venous thromboembolism (VTE).

SSR-126517, a biotinylated idraparinux, had been in phase III clinical trials at Sanofi (formerly known as sanofi-aventis) for the treatment of pulmonary embolism, deep venous thrombosis (DVT) and atrial fibrillation. However, in 2009, development of the compound was discontinued.


Idrabiotaparinux (biotinylated idraparinux, SSR-126517, SSR-126517E) is a long-acting selective pentasaccharide indirect factor Xa coagulation inhibitor, administered by…

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