Activators & Inhibitors

Sitagliptin (MK0431), a new oral hypoglycemic (anti-diabetic drug), is a new dipeptidyl peptidase-4 (DPP-4) inhibitor. This enzyme-inhibiting drug is used either alone or in combination with metformin or thiazolidinedione for treatment of type 2 diabetes mellitus. The drug can competitively inhibit a protein/enzyme and DPP-4, that leads to an incremental amount of active incretins (GLP-1 and GIP), the diminished amount of release of glucagon and increased release of insulin.

Vanitiolide (Vanitiolid) has cholelitic effects.

Tilorone dihydrochloride, an orally active interferon inducer, exhibits both antineoplastic and anti-inflammatory actions.

RS 61443 (Mycophenolate mofetil) is an immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH)

Betahistine dihydrochloride (Betahistine 2HCl) is a histamine analog and H1 receptor agonist that serves as a vasodilator.

Betahistine mesylate (Extovyl) is a histamine analog and H1 receptor agonist that serves as a vasodilator. It is used in MENIERE DISEASE and in vascular headaches but may exacerbate bronchial asthma and peptic ulcers.

Acarbose (BAY g 5421) is an inhibitor of α-Glucosidases with antihyperglycemic activity.

Clorprenaline hydrochloride (Clorprenaline HCl) is a beta-2 adrenergic agonist with bronchodilator activity.

N-Acetylprocainamide (NAPA), the N-acetylated metabolite of Procainamide, is a Class III antiarrhythmic agent, while procainamide is a Class Ia antiarrhythmic drug.