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Candesartan Cilexetil
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Candesartan Cilexetil is an angiotensin II receptor antagonist with actions similar to those of losartan (Losartan Potassium). It is used in the management of hypertension and may also be used in heart failure in patients with impaired left ventricular systolic function, either when ACE inhibitors are not tolerated, or in addition to ACE inhibitors. Candesartan Cilexetil's originator is Takeda, and it is marketed worldwide by AstraZeneca under brand names of ATACAND and ATACAND HCTZ and by Takeda under brand names of Blopress and Blopress Plus. Candesartan Cilexetil is a prodrug which hydrolyzed to Candesartan during absorption from the gastrointestinal tract. Candesartan Cilexetil is rapidly and completely bioactivated by ester hydrolysis during absorption from the gastrointestinal tract to Candesartan, a selective AT 1 subtype angiotensin II receptor antagonist Candesartan Cilexetil appears in plain tablets ( 4mg, 8 mg, 16mg, 32 mg) or in combination tablets with hydrochlorothiazide (16mg /12.5mg HCTZ, 32mg /12.5mg HCTZ ) administrated once daily. Following administration of the prodrug, the absolute bioavailability of Candesartan was estimated to be 15%.
Candesartan Cilexetil's plain tablets are on the market since 1997 and the combination tablets with HCTZ are marketed since 1998.
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General data on Candesartan Cilexetil Active Pharmaceutical Ingredient
CAS Registry: 139481-59-7 (candesartan); 145040-37-5 (candesartan cilexetil)
ATC:C09CA06
Molecular Formula: C33H34N6O6
Molecular Weight: 610.7
Candesartan Cilexetil Active Pharmaceutical Ingredient is a white to off-white powder. It is practically insoluble in water and sparingly soluble in methanol. Candesartan cilexetil is a racemic mixture containing one chiral center at the cyclohexyloxycarbonyloxy ethyl ester group.
TAPI's Candesartan Cilexetil Pharmaceutical Ingredient
TAPI's Candesartan Cilexetil Active Pharmaceutical Ingredient is produced in Assia Industries Limited –Teva Tech site in Beer Sheva, Israel.
Candesartan Cilexetil produced by TAPI by organic synthesis and considered to be medium volume Active Pharmaceutical Ingredient.
TAPI's product has unique features that might be advantage for final dosage development. TAPI has filed several patent applications for Candesartan Cilexetil. Please, see table below for issued patents and pending applications.
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Patent type |
Description |
App./publication/patent # |
Status (date) |
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Process |
Preparation of candesartan |
US 7,098,342 |
Issued
29/8/2006 |
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WO 2005037821 |
Pending
28/04/2005 |
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EP 1,685,126 |
Issued |
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US 20060252939 |
Pending
09/11/2006 |
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Polymorphic form |
Candesartan cilexetil polymorphs |
US 20050250828 |
Pending
10/11/2005 |
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WO 2005077941 |
Pending
25/08/2005 |
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Impurity |
Pure Candesartan |
US 20050250827 |
Pending
10/11/2005 |
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WO 2005111021 |
Pending
24/11/2005 |
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Process |
Preparation of crude candesartan |
WO 2006076710 |
Pending
20/7/2006 |
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US 20060194858 |
Pending
31/8/2006 |
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Stability |
Stable micronized Candesartan colixetil |
WO 2006122254 |
Pending
16/11/2006 |
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US20070082055 |
Pending
12/04/2007 | |
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2008 Available DMF: USDMF
TAPI provide full service on this product and other APIs in our portfolio. Our local sales offices provide full information on our product, regulatory compliance and documentation on Candesartan Cilexetil. Contact us today for further inquiries and samples and kilograms availability information for TAPI's Candesartan Cilexetil.
Other products, in the group of Angiotensin II Antagonists, available on TAPI's portfolio are: Losartan Potasium, Valsartan, Irbesartan, Telmisartan and Olmesartan Medoxomil. Contact us today for information on these products.
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Legal Note
Product exploitation, including development, sales and offer for sale are performed where permissible by patent law. This presentation is not and should not constitute an offer for sale in territories where it is not permitted by law. In USA Products that Currently on Patent are available for R&D Use in Accordance with 35 USC §271 (e) (1).
*TAPI stands for Teva's Active Pharmaceutical Ingredients
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