Aflibercept


Generic Medicine Info
Indications and Dosage
Intravenous
Metastatic colorectal cancer
Adult: In combination with folinic acid, fluorouracil, and irinotecan (FOLFIRI) in patients with resistance to or progression after an oxaliplatin-containing regimen: 4 mg/kg every 2 weeks given via infusion over 1 hour. Continue until disease progression or unacceptable toxicity. Dose may be withheld or discontinued based on patient safety and tolerability (refer to detailed product guideline).

Intravitreal
Myopic choroidal neovascularisation
Adult: 2 mg as a single dose, additional doses may be given at least 1 month apart if needed.

Intravitreal
Macular oedema secondary to retinal vein occlusion
Adult: Initially, 2 mg once monthly until max visual acuity is achieved and no signs of disease activity. Treatment interval may gradually increase to maintain stable visual and anatomic outcomes or shorten if deterioration occurs. Discontinue if no improvement.

Intravitreal
Neovascular (wet) age-related macular degeneration
Adult: Initially, 2 mg once monthly for 3 consecutive months, followed by 2 mg once every 2 months; some patients may need to continue monthly dosing for a longer period. After 12 months of treatment, doses may be given less frequently according to response and intervals should be shortened again if deterioration occurs.

Intravitreal
Diabetic macular oedema, Diabetic retinopathy
Adult: Initially, 2 mg once monthly for 5 months, followed by 2 mg once every 2 months; some patients may need to continue monthly dosing for a longer period. After 12 months of treatment, doses may be given less frequently according to response and intervals should be shortened again if deterioration occurs.
Reconstitution
IV: Dilute with 5% dextrose injection or 0.9% NaCl to a final concentration of 0.6-8 mg/mL.
Contraindications
IV: NYHA class III or IV CHF, uncontrolled hypertension, severe haemorrhage. Intravitreal: Active or suspected ocular/periocular infection, active severe intraocular inflammation, clinical signs of irreversible ischaemic visual function loss.
Special Precautions
Patient with history of CV disease (e.g. coronary artery disease, CHF); poorly controlled glaucoma (intravitreal). Patient undergoing surgery. Elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Arterial thromboembolic events (e.g. TIA, CVA, angina; nonfatal stroke and MI), hypersensitivity reactions. IV: Bone marrow suppression (e.g. neutropenia, leucopenia, thrombocytopenia), venous thromboembolic events (e.g. deep vein thrombosis), cardiac failure, decreased ejection fraction, aneurysms, artery dissections, severe diarrhoea, dehydration, gastrointestinal or non-gastrointestinal fistula, hypertension, proteinuria, impaired wound healing, osteonecrosis of the jaw. Intravitreal: Endophthalmitis, rhegmatogenous retinal detachment, retinal tear, retinal pigment epithelium tear, iatrogenic traumatic cataract, intraocular inflammation, increased intraocular pressure, immunogenicity.
Blood and lymphatic system disorders: Febrile neutropenia.
Eye disorders: Eye pain, reduced visual acuity, blurred vision, retinal/conjunctival haemorrhage; retinal pigment epithelium detachment, retinal degeneration; vitreous haemorrhage, floaters, or detachment; cataract (e.g. cotical, nuclear, subscapular); corneal erosion or abrasion; foreign body sensation, increased lacrimation, eyelid oedema, punctate keratitis, conjunctival/ocular hyperaemia.
Gastrointestinal disorders: Stomatitis, aphthous stomatitis, toothache, abdominal pain, rectal haemorrhage, proctalgia.
General disorders and administration site conditions: Asthenia, injection site haemorrhage.
Infections and infestations: Infection, sepsis.
Investigations: Weight loss, increased AST/ALT, creatinine.
Metabolism and nutrition disorders: Decreased appetite.
Nervous system disorders: Headache.
Renal and urinary disorders: Urinary tract infection.
Respiratory, thoracic and mediastinal disorders: Nasopharyngitis, epistaxis, oropharyngeal pain, rhinorrhoea.
Skin and subcutaneous tissue disorders: Palmar-plantar erythrodysaesthesia syndrome, skin hyperpigmentation.
Potentially Fatal: IV: Severe haemorrhage, gastrointestinal perforation or bleeding, reversible posterior leukoencephalopathy syndrome, pulmonary embolism.
Intravitreal/IV: C
Patient Counseling Information
This drug may cause temporary visual disturbance after intravitreal injection, if affected, do not drive or operate machinery.
MonitoringParameters
IV: Perform Hepatitis B virus screening with hepatitis B surface antigen (HBsAg), hepatitis B core antibody (anti-HBc), and antibody to hepatitis B surface antigen (anti-HBs) before treatment. Monitor CBC with differential at baseline and prior to each cycle; urine protein, blood pressure (every 2 weeks and as indicated), wounds for healing impairment. Perform pregnancy test to women of child-bearing potential prior to initiation of therapy. Monitor for signs and symptoms of haemorrhage, gastrointestinal perforation; diarrhoea, dehydration (elderly). Intravitreal: Monitor intraocular pressure, optic nerve head perfusion, visual acuity. Monitor for signs and symptoms of intraocular inflammation (e.g. pain, photophobia or redness), infection, endophthalmitis, retinal detachment.
Action
Description: Aflibercept is a recombinant fusion protein that acts as a soluble decoy receptor and binds to vascular endothelial growth factor VEGF-A and -B, and placental growth factor (PlGF). Thus, preventing the activation of receptor tyrosine kinases VEGF-1 and VEGFR-2 and the proliferation of endothelial cells, thereby inhibiting the growth of new vessels.
Pharmacokinetics:
Absorption: Slowly absorbed after intravitreal administration. Time to peak plasma concentration: Within 3 days.
Distribution: Volume of distribution: Approx 6 L (IV).
Excretion: Elimination half-life: Approx 6 days (IV).
Storage
Store between 2-8°C. Do not freeze. Protect from light. This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
ATC Classification
S01LA05 - aflibercept ; Belongs to the class antineovasculatisation agents. Used in the management of neovascular macular degeneration.
L01XX44 - aflibercept ; Belongs to the class of other antineoplastic agents. Used in the treatment of cancer.
References
Anon. Aflibercept (EENT). AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 09/11/2020.

Anon. Aflibercept (Ophthalmic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 09/11/2020.

Anon. Aflibercept (Systemic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 09/11/2020.

Anon. Ziv-Aflibercept. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 09/11/2020.

Buckingham R (ed). Aflibercept. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/11/2020.

Eylea 40 mg/mL Solution for Injection (Regeneron Pharmaceuticals, Inc. Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my/. Accessed 09/11/2020.

Eylea Injection, Solution (Regeneron Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 09/11/2020.

Joint Formulary Committee. Aflibercept. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/11/2020.

Zaltrap 25 mg/mL Concentrate for Solution for Infusion (Sanofi-Aventis Deutschland GmbH Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my/. Accessed 09/11/2020.

Zaltrap Solution, Concentrate (Sanofi-Aventis U.S. LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 09/11/2020.

Disclaimer: This information is independently developed by MIMS based on Aflibercept from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 MIMS. All rights reserved. Powered by MIMS.com
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