DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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Health Canada approves Forest Laboratories Bystolic
The chemical name for the active ingredient in BYSTOLIC (nebivolol) tablets is (1RS,1’RS)-1,1′-[(2RS,2’SR)bis(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl)]-2,2′-iminodiethanol hydrochloride. Nebivolol is a racemate composed of d-Nebivolol and l-Nebivolol with the stereochemical designations of [SRRR]-nebivolol and [RSSS]nebivolol, respectively. Nebivolol’s molecular formula is (C22H25F2NO4•HCl) with the following structural formula:
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SRRR – or d-nebivolol hydrochloride
RSSS – or l-nebivolol hydrochloride
MW: 441.90 g/mol
Nebivolol hydrochloride is a white to almost white powder that is soluble in methanol, dimethylsulfoxide, and N,N-dimethylformamide, sparingly soluble in ethanol, propylene glycol, and polyethylene glycol, and very slightly soluble in hexane, dichloromethane, and methylbenzene.
BYSTOLIC as tablets for oral administration contains nebivolol hydrochloride equivalent to 2.5, 5, 10, and 20 mg of nebivolol base. In addition, BYSTOLIC contains the following inactive ingredients: colloidal silicon dioxide, croscarmellose sodium, D&C Red #27 Lake, FD&C Blue #2 Lake, FD&C Yellow #6 Lake, hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, pregelatinized starch, polysorbate 80, and sodium lauryl sulfate.
Class: beta-Adrenergic Blocking Agents
Chemical Name: (1RS,1′RS)-1,1′-[(2RS,2′SR)-bis(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl)]- 2,2′-iminodiethanol hydrochloride
Molecular Formula: C22H25F2NO4•HCl
CAS Number: 152520-56-4
Brands: Bystolic
Health Canada has issued a notice of compliance for Forest Laboratories Canada’s hypertension therapy, Bystolic (nebivolol) tablets.
The company anticipates making the hypertension medication, that is to be administered once a day, available to patients across Canada in the second quarter of 2013.
Forest Laboratories corporate development and strategic planning senior vice president David Solomon said, “We are pleased that Health Canada has granted approval for BYSTOLIC. This is an important milestone for Forest, as it is the first product approved for our newly established Canadian subsidiary.”
Nebivolol is a beta adrenergic receptor blocking agent which is metabolized by various routes such as glucuronidation and hydroxylation by CYP2D6.
Possible factors that allow Bystolic to act as antihypertensive agent include decreased heart rate, decreased myocardial contractility, diminution of tonic sympathetic outflow to the periphery from cerebral vasomotor centers, suppression of renin activity and vasodilation and decreased peripheral vascular resistance.
New Drug Approvals 