Product Information
Registration Status: ActiveEMGALITY SOLUTION FOR INJECTION IN PRE-FILLED SYRINGE 100 MG/ML is approved to be sold in Singapore with effective from 2020-12-18. It is marketed by ELI LILLY (SINGAPORE) PTE LTD, with the registration number of SIN16063P.
This product contains Galcanezumab 100mg/ml in the form of INJECTION, SOLUTION. It is approved for SUBCUTANEOUS use.
This product is manufactured by Eli Lilly and Company 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
LY2951742/galcanezumab is a fully humanized monoclonal antibody against human calcitonin gene-related peptide (CGRP) that is developed by ELi Lilly and Company [A33105]. This therapy is given as a single subcutaneous injection twice a month and ongoing clinical trials for the agent are for episodic and chronic migraine as well as cluster headaches [A33114].
Indication
Galcanezumab is a humanized monoclonal antibody that may be effective in migraine prophylaxis by binding endogenous human calcitonin gene-related peptide (CGRP) [A33112].
Mechanism of Action
Galcanezumab is a fully humanized monoclonal antibody designed and manufactured specifically against calcitonin gene-related peptide (CGRP) [A33105]. It binds avidly to human CGRP, with a binding affinity (Kd) of 31 pM (4.5 ng/mL). 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 of CGRP to interfere with its activity was specifically designed to be the form and mechanism of action for galcanezumab to take advantage of in reversing the migraine-inducing activity of natural CGRP. The binding of galcanezumab to natural endogenous CGRP subsequently interferes with its activities, such as its binding to CGRP receptors, for example. Studies have also shown that humanized monoclonal antibodies against CGRP have proven successful in reducing the frequency of migraine headaches in early clinical trials as a preventative therapeutic [A33112].
Pharmacokinetics
- Absorption
- Following single dose subcutaneous administration, there appeared to be an extended period of absorption, with a median time to peak concentration (Tmax) between Days 7 and 14 [A33112]. Cmax and the area under the concentration-time curve from dosing to infinity (AUC (0-∞)) are generally considered to be dose proportional over a dose range [A33112].
- Distribution
- Readily accessible data regarding the volume of distribution of galcanezumab is not available.
- Metabolism
- Monoclonal antibody agents like galcanezumab are not expected to generate toxic metabolites as they generally undergo proteolysis to their constituent amino acids [F94].
- Elimination
Clearance
It is noted that the clearance of galcanezumab is by proteolysis [A33112].
Toxicity
The most common adverse effects associated with galcanezumab during clinical trials include headache, nasopharyngitis, hematuria, and contact dermatitis [A33112]. However, with the exception of hematuria which was not present in placebo treatment arms, the frequencies of these events were similar to placebo [A33112]. Additional frequently reported adverse effects in subjects receiving galcanezumab were diarrhea, toothache, and increased alanine aminotransferase (ALT) [A33112].
Active Ingredient/Synonyms
Galcanezumab | Galcanezumab |
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.