TABLE 5 | Protein therapeutics providing a novel function or activity (Group Ic)
From the following article:
Protein therapeutics: a summary and pharmacological classification
Benjamin Leader, Quentin J. Baca & David E. Golan
Nature Reviews Drug Discovery 7, 21-39 (January 2008)
doi:10.1038/nrd2399
| Therapeutic | Trade name | Function | Examples of clinical use |
|---|---|---|---|
| Enzymatic degradation of macromolecules | |||
| * Botulinum toxin type A232, 233 | Botox | Cleaves SNAP25 at neuromuscular junctions to disrupt SNARE complex and prevent acetylcholine release, causing flaccid paralysis | Many types of dystonia, particularly cervical; cosmetic uses |
| *Botulinum toxin type B233, 234 | Myoblock | Cleaves synaptobrevin at neuromuscular junctions to disrupt SNARE complex and prevent acetylcholine release, causing flaccid paralysis | Many types of dystonia, particularly cervical; cosmetic uses |
| *Collagenase56, 57 | Collagenase, Santyl | Collagenase obtained from fermentation by Clostridium histolyticum; digests collagen in necrotic base of wounds | Debridement of chronic dermal ulcers and severely burned areas |
Human deoxy-ribonuclease I, dornase- 58 | Pulmozyme | Degrades DNA in purulent pulmonary secretions | Cystic fibrosis; decreases respiratory tract infections in selected patients with FVC greater than 40% of predicted |
| *Hyaluronidase (bovine, ovine)235 | Amphadase (bovine), Hydase (bovine), Vitrase (ovine) | Catalyses the hydrolysis of hyaluronic acid to increase tissue permeability and allow faster drug absorption | Used as an adjuvant to increase the absorption and dispersion of injected drugs, particularly anaesthetics in ophthalmic surgery and certain imaging agents |
| Hyaluronidase (recombinant human)236 | Hylenex | Catalyses the hydrolysis of hyaluronic acid to increase tissue permeability and allow faster drug absorption | Used as an adjuvant to increase the absorption and dispersion of injected drugs, particularly anaesthetics in ophthalmic surgery and certain imaging agents |
| *Papain55 | Accuzyme, Panafil | Protease from the Carica papaya fruit | Debridement of necrotic tissue or liquefication of slough in acute and chronic lesions, such as pressure ulcers, varicose and diabetic ulcers, burns, postoperative wounds, pilonidal cyst wounds, carbuncles, and other wounds |
| Enzymatic degradation of small-molecule metabolites | |||
| *L-Asparaginase60 | ELSPAR | Provides exogenous asparaginase activity, removing available asparagine from serum; purified from Escherichia coli | Acute lymphocytic leukaemia, which requires exogenous asparagine for proliferation |
| *Peg-asparaginase59 | Oncaspar | Provides exogenous asparaginase activity, removing available asparagine from serum; purified from E. coli | Acute lymphocytic leukaemia, which requires exogenous asparagine for proliferation |
| Rasburicase237 | Elitek | Catalyzes enzymatic oxidation of uric acid into an inactive, soluble metabolite (allantoin); originally isolated from Aspergillus flavus | Paediatric patients with leukaemia, lymphoma, and solid tumours who are undergoing anticancer therapy that may cause tumour lysis syndrome |
| Haemostasis and thrombosis | |||
| Lepirudin61, 62 | Refludan | Recombinant hirudin, a thrombin inhibitor from the salivary gland of the medicinal leech Hirudo medicinalis | Heparin-induced thrombocytopaenia |
| ‡Bivalirudin238, 239 | Angiomax | Synthetic hirudin analogue; specifically binds both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin | Reduce blood-clotting risk in coronary angioplasty and heparin-induced thrombocytopaenia |
| *Streptokinase63, 64, 65, 240 | Streptase | Converts plasminogen to plasmin; produced by group C b-haemolytic streptococci | Acute evolving transmural myocardial infarction, pulmonary embolism, deep vein thrombosis, arterial thrombosis or embolism, occlusion of arteriovenous cannula |
| *Anistreplase241, 242 (anisoylated plasminogen streptokinase activator complex; APSAC) | Eminase | Converts plasminogen to plasmin; p-anisoyl group protects the catalytic centre of the plasminogen-streptokinase complex and prevents premature deactivation, thereby providing longer duration of action than streptokinase | Thrombolysis in patients with unstable angina |
| Protein therapeutics are recombinant unless otherwise stated.*Non-recombinant.‡Synthetic. FVC, forced vital capacity; SNAP25, synaptosomal-associated protein, 25 kDa; SNARE, soluble N-ethylmaleimide-sensitive factor attachment protein receptor. | |||
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