Product Information
Registration Status: ActiveAIMOVIG SOLUTION FOR INJECTION IN PRE-FILLED PEN 140MG/ML is approved to be sold in Singapore with effective from 2020-04-03. It is marketed by NOVARTIS (SINGAPORE) PTE LTD, with the registration number of SIN15925P.
This product contains Erenumab 140 MG/ML in the form of INJECTION, SOLUTION. It is approved for SUBCUTANEOUS use.
This product is manufactured by Amgen Manufacturing Limited (Bulk Production/Primary Packaging) in UNITED STATES.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Erenumab (AMG-334) (INN; trade name Aimovig) is a human monoclonal antibody designed specifically to bind and antagonize the calcitonin gene-related peptide receptor (CGRPR) as a means to prevent migraines. Aimovig, as released and marketed by Novartis and Amgen, is in fact a novel therapeutic approach as the first and only FDA approved treatment specifically developed to prevent migraine by blocking the CGRP receptor, which is believed to play a critical role in migraine [L2823]. In particular, erenumab-aooe is a human immunoglobulin G2 monoclonal antibody that has high affinity binding to the CGRP receptor [FDA Label]. The antibody is produced utlilizing recombinant DNA technology in Chinese hamster ovary cells [FDA Label]. It is composed of 2 heavy chains, each containing 456 amino acids, and 2 light chains of the lambda subclass, each containing 216 amino acids, with an approximate molecular weight of 150 kDa [FDA Label].
Indication
Erenumab is indicated for the preventative treatment of migraine in adults [FDA Label].
Mechanism of Action
Erenumab is a human monoclonal antibody that has been designed to bind specifically to the calcitonin gene-related peptide (CGRP) receptor and antagonize the CGRP receptor function [FDA Label]. Studies since 1985 have demonstrated that CGRP levels increase during acute migraine attacks in migraine-suffering patients but normalize after efficacious sumatriptan therapy [A33090]. Moreover, research has also shown that intravenous administration of CGRP can induce migraine-like attacks in migraine-suffering patients [A33090]. For all these reasons, the binding and antagonism of CGRP receptors was designed to be mechanism of action for erenumab to take advantage of in reversing the migraine-inducing activity of natural CGRP. CGRP and its receptor are expressed in both the peripheral and the central nervous system [A33091]. In addition to playing a role in cranial nociception, CGRP is also a potent general arterial vasodilator [A33091]. At peripheral synapses, CGRP released from trigeminal terminals results in vasodilation via CGRP receptors on the smooth muscle cells of meningeal and cerebral blood vessels [A33090].
Pharmacokinetics
- Absorption
- Following a single subcutaneous dose of 70 mg or 140 mg erenumab administered to healthy adults, the median peak serum concentrations were attained in about 6 days, and the estimated absolute bioavailability was approximately 82% [FDA Label].
- Distribution
- After a single 140 mg intravenous dose, the mean (SD) volume of distribution during the terminal phase (Vz) was estimated to be approximately 3.86 (0.77) L [FDA Label].
- Metabolism
- Erenumab CGRP antibodies demonstrate a low risk for drug-drug interactions and hepatotoxicity since they are predominantly metabolized by degradation into peptides and single amino acids [A33090].
- Elimination
Clearance
Certain studies show that the population estimate of linear clearance is independent of erenumab concentrations and stays approximately constant at 0.214 L/day (95% CI: 0.191–0.243) [A33091]. In contrast, the nonlinear clearance is dependent on the target receptor density and the amount of erenumab bound to the receptors [A33091]. Nevertheless, the maximal nonlinear clearance was observed to be about 1.84L/day [A33091].
Toxicity
The most common side effects of erenumab include pain, redness, or swelling at the injection site, and constipation. Information regarding overdosage is not available [FDA Label].
Active Ingredient/Synonyms
Erenumab | Erenumab |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.