Evolocumab

Subcutaneous
Heterozygous familial hypercholesterolaemia, Mixed dyslipidaemia, Nonfamilial hypercholesterolaemia

Subcutaneous
Familial homozygous hypercholesterolaemia

Pregnancy and lactation. Renal and hepatic impairment.

Significant: Hypersensitivity reactions (e.g. rash, urticaria).
Gastrointestinal disorders: Nausea, diarrhoea, gastroenteritis.
General disorders and administration site conditions: Inj site reactions.
Infections and infestations: Influenza.
Musculoskeletal and connective tissue disorders: Back pain, arthralgia, myalgia.
Nervous system disorders: Headache, dizziness.
Renal and urinary disorders: UTI.
Respiratory, thoracic and mediastinal disorders: Nasopharyngitis, upper respiratory infection, cough, sinusitis.
Vascular disorders: Hypertension.

Monitor lipid profile; LDL-C levels 4-8 weeks after initiation of treatment (in patients with homozygous familial hypercholesterolaemia); signs and symptoms of hypersensitivity.

Description:
Mechanism of Action: Evolocumab is a human monoclonal antibody (IgG2 isotype) that binds to proprotein convertase subtilisin kexin type 9 (PCSK9). It inhibits PCSK9 from binding to LDL receptors in the liver thereby increasing receptor numbers, leading to increased uptake of LDL-cholesterol hence lowering its level in the blood.
Onset: Proprotein convertase subtilisin kexin type 9 (PCSK9) suppression: 4 hours.
Pharmacokinetics:
Absorption: Bioavailability: 72%. Time to peak plasma concentration: 3-4 days.
Distribution: Volume of distribution: Approx 3.3 L.
Metabolism: Metabolised via nonsaturable proteolytic pathway.
Excretion: Elimination half-life: 11-17 days.

Store between 2-8°C. Protect from light. Do not freeze. Any unused portions should be disposed of in accordance with local requirements.

Dyslipidaemic Agents

C10AX13 - evolocumab ; Belongs to the class of other lipid modifying agents.

Anon. Evolocumab. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com/. Accessed 30/01/2018.

Anon. Evolocumab. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 30/01/2018.

Buckingham R (ed). Evolocumab. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/01/2018.

Joint Formulary Committee. Evolocumab. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/01/2018.

Repatha Injection, Solution (Amgen Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 30/01/2018.