Peringatan Keamanan

Toxicity information regarding galcanezumab is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as nasopharyngitis, hematuria, and contact dermatitis.A33112 Symptomatic and supportive measures are recommended. Additional adverse effects reported in healthy subjects receiving a single high dose of galcanezumab (600 mg) were diarrhea, vomiting and high levels of alanine aminotransferase.A33112

Studies evaluating the carcinogenic potential or genetic toxicology of galcanezumab have not yet been conducted.L42060 No adverse effects were observed in male rats given galcanezumab (0, 30, or 250 mg/kg) subcutaneously before or during mating. The highest dose given to male rats corresponded to 8 or 4 times the recommended human dose for migraine (120 mg) or episodic cluster headache (300 mg), respectively.L42060 Female rats given 0, 30, 100 or 250 mg/kg of galcanezumab did not show adverse effects on fertility either. The highest dose given to female rats corresponded to 38 or 18 times the recommended human dose for migraine (120 mg) or episodic cluster headache (300 mg), respectively.L42060

Galcanezumab

DB14042

biotech approved investigational

Deskripsi

Galcanezumab is a humanized monoclonal antibody developed by Eli Lilly and Company against human calcitonin gene-related peptide (CGRP).A33105 Although several small-molecule CGRP receptor antagonists have been developed, humanized monoclonal antibodies like galcanezumab are specifically designed to selectively bind to CGRP entities with high potency.A33112 Given this target specificity, lack of off-target toxicity, and characteristic proteolysis profile of immunoglobulin antibodies to not undergo metabolism by liver enzymes, galcanezumab possesses favourable and promising safety and tolerability.A33112 Galcanezumab was approved by the FDA in September 2018, and is indicated for the preventive treatment of migraine and the treatment of episodic cluster headache.L42060 It is unknown if galcanezumab has an effect on pregnancy outcomes. A pregnancy exposure registry has been established to evaluate the safety of this drug in pregnant women.L42060

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Between 1 and 600 mg of galcanezumab, the mean serum half-life ranged from 25 to 30 days.[A33112] On average, the elimination half-life of galcanezumab was approximately 27 days.[L42060]
Volume Distribusi The apparent volume of distribution of galcanezumab is 7.3 L, with 34% inter-individual variability.[L42060]
Klirens (Clearance) The apparent clearance of galcanezumab is 0.008 L/h.[L42060]

Absorpsi

Galcanezumab follows a linear pharmacokinetic profile, with a Cmax and AUC0-? considered to be dose-proportional between 1 and 600 mg.A33112,L42060 After a single dose of galcanezumab-gnlm administered subcutaneously, the time to maximum concentration was 5 days.L42060 In a group of healthy subjects (n=7) given four biweekly doses of galcanezumab, Tmax was 3 days, Cmax was 37,210 ng/mL and the AUC was 1,959,000 ng?day/mL.A33112 The injection site location does not appear to significantly influence the absorption of this drug.L42060 Galcanezumab is expected to have a subcutaneous bioavailability between 50% and 100%, similar to other monoclonal antibodies.A249000 Renal and hepatic impairment are not expected to have an effect on the pharmacokinetics of galcanezumab. A population analysis has shown that pharmacokinetic parameters are not affected by age, sex, race, or subtypes of migraine spectrum (episodic or chronic migraine), while body weight has no clinically relevant effect on the pharmacokinetics of galcanezumab.L42060

Metabolisme

After administration, galcanezumab is expected to be degraded into small peptides and amino acids by proteolysis, in a process similar to the one followed by endogenous immunoglobulins.L42060 Galcanezumab is not believed to be metabolized by liver enzymes, making drug-drug interactions relatively unlikely.L42060

Rute Eliminasi

Monoclonal antibody agents like galcanezumab are generally eliminated via intracellular catabolism, followed by fluid-phase or receptor-mediated endocytosis.A249000

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with or without food.

Interaksi Obat

373 Data
Diethylstilbestrol Diethylstilbestrol may increase the thrombogenic activities of Galcanezumab.
Chlorotrianisene Chlorotrianisene may increase the thrombogenic activities of Galcanezumab.
Conjugated estrogens Conjugated estrogens may increase the thrombogenic activities of Galcanezumab.
Estrone Estrone may increase the thrombogenic activities of Galcanezumab.
Estradiol Estradiol may increase the thrombogenic activities of Galcanezumab.
Dienestrol Dienestrol may increase the thrombogenic activities of Galcanezumab.
Ethinylestradiol Ethinylestradiol may increase the thrombogenic activities of Galcanezumab.
Mestranol Mestranol may increase the thrombogenic activities of Galcanezumab.
Estriol Estriol may increase the thrombogenic activities of Galcanezumab.
Estrone sulfate Estrone sulfate may increase the thrombogenic activities of Galcanezumab.
Quinestrol Quinestrol may increase the thrombogenic activities of Galcanezumab.
Hexestrol Hexestrol may increase the thrombogenic activities of Galcanezumab.
Tibolone Tibolone may increase the thrombogenic activities of Galcanezumab.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may increase the thrombogenic activities of Galcanezumab.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may increase the thrombogenic activities of Galcanezumab.
Polyestradiol phosphate Polyestradiol phosphate may increase the thrombogenic activities of Galcanezumab.
Esterified estrogens Esterified estrogens may increase the thrombogenic activities of Galcanezumab.
Zeranol Zeranol may increase the thrombogenic activities of Galcanezumab.
Equol Equol may increase the thrombogenic activities of Galcanezumab.
Promestriene Promestriene may increase the thrombogenic activities of Galcanezumab.
Methallenestril Methallenestril may increase the thrombogenic activities of Galcanezumab.
Epimestrol Epimestrol may increase the thrombogenic activities of Galcanezumab.
Moxestrol Moxestrol may increase the thrombogenic activities of Galcanezumab.
Estradiol acetate Estradiol acetate may increase the thrombogenic activities of Galcanezumab.
Estradiol benzoate Estradiol benzoate may increase the thrombogenic activities of Galcanezumab.
Estradiol cypionate Estradiol cypionate may increase the thrombogenic activities of Galcanezumab.
Estradiol valerate Estradiol valerate may increase the thrombogenic activities of Galcanezumab.
Biochanin A Biochanin A may increase the thrombogenic activities of Galcanezumab.
Formononetin Formononetin may increase the thrombogenic activities of Galcanezumab.
Estetrol Estetrol may increase the thrombogenic activities of Galcanezumab.
Cetuximab The risk or severity of adverse effects can be increased when Cetuximab is combined with Galcanezumab.
Human immunoglobulin G The risk or severity of adverse effects can be increased when Human immunoglobulin G is combined with Galcanezumab.
Omalizumab The risk or severity of adverse effects can be increased when Omalizumab is combined with Galcanezumab.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Galcanezumab.
Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Galcanezumab.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Galcanezumab.
Indium In-111 satumomab pendetide The risk or severity of adverse effects can be increased when Indium In-111 satumomab pendetide is combined with Galcanezumab.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Galcanezumab.
Trastuzumab The risk or severity of adverse effects can be increased when Trastuzumab is combined with Galcanezumab.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Galcanezumab.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Galcanezumab.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Galcanezumab.
Digoxin Immune Fab (Ovine) The risk or severity of adverse effects can be increased when Digoxin Immune Fab (Ovine) is combined with Galcanezumab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Galcanezumab.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Galcanezumab.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Galcanezumab.
Capromab pendetide The risk or severity of adverse effects can be increased when Capromab pendetide is combined with Galcanezumab.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Galcanezumab.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Galcanezumab.
Natalizumab The risk or severity of adverse effects can be increased when Natalizumab is combined with Galcanezumab.
Palivizumab The risk or severity of adverse effects can be increased when Palivizumab is combined with Galcanezumab.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Galcanezumab.
Bevacizumab The risk or severity of adverse effects can be increased when Bevacizumab is combined with Galcanezumab.
Technetium Tc-99m arcitumomab The risk or severity of adverse effects can be increased when Technetium Tc-99m arcitumomab is combined with Galcanezumab.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Galcanezumab.
Panitumumab The risk or severity of adverse effects can be increased when Panitumumab is combined with Galcanezumab.
Ranibizumab The risk or severity of adverse effects can be increased when Ranibizumab is combined with Galcanezumab.
Galiximab The risk or severity of adverse effects can be increased when Galiximab is combined with Galcanezumab.
Pexelizumab The risk or severity of adverse effects can be increased when Pexelizumab is combined with Galcanezumab.
Afelimomab The risk or severity of adverse effects can be increased when Afelimomab is combined with Galcanezumab.
Epratuzumab The risk or severity of adverse effects can be increased when Epratuzumab is combined with Galcanezumab.
Bectumomab The risk or severity of adverse effects can be increased when Bectumomab is combined with Galcanezumab.
Oregovomab The risk or severity of adverse effects can be increased when Oregovomab is combined with Galcanezumab.
IGN311 The risk or severity of adverse effects can be increased when IGN311 is combined with Galcanezumab.
Adecatumumab The risk or severity of adverse effects can be increased when Adecatumumab is combined with Galcanezumab.
Labetuzumab The risk or severity of adverse effects can be increased when Labetuzumab is combined with Galcanezumab.
Matuzumab The risk or severity of adverse effects can be increased when Matuzumab is combined with Galcanezumab.
Fontolizumab The risk or severity of adverse effects can be increased when Fontolizumab is combined with Galcanezumab.
Bavituximab The risk or severity of adverse effects can be increased when Bavituximab is combined with Galcanezumab.
CR002 The risk or severity of adverse effects can be increased when CR002 is combined with Galcanezumab.
Rozrolimupab The risk or severity of adverse effects can be increased when Rozrolimupab is combined with Galcanezumab.
Girentuximab The risk or severity of adverse effects can be increased when Girentuximab is combined with Galcanezumab.
Obiltoxaximab The risk or severity of adverse effects can be increased when Obiltoxaximab is combined with Galcanezumab.
XTL-001 The risk or severity of adverse effects can be increased when XTL-001 is combined with Galcanezumab.
NAV 1800 The risk or severity of adverse effects can be increased when NAV 1800 is combined with Galcanezumab.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Galcanezumab.
Otelixizumab The risk or severity of adverse effects can be increased when Otelixizumab is combined with Galcanezumab.
AMG 108 The risk or severity of adverse effects can be increased when AMG 108 is combined with Galcanezumab.
Iratumumab The risk or severity of adverse effects can be increased when Iratumumab is combined with Galcanezumab.
Enokizumab The risk or severity of adverse effects can be increased when Enokizumab is combined with Galcanezumab.
Ramucirumab The risk or severity of adverse effects can be increased when Ramucirumab is combined with Galcanezumab.
Farletuzumab The risk or severity of adverse effects can be increased when Farletuzumab is combined with Galcanezumab.
Veltuzumab The risk or severity of adverse effects can be increased when Veltuzumab is combined with Galcanezumab.
Ustekinumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Galcanezumab.
Trastuzumab emtansine The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Galcanezumab.
PRO-542 The risk or severity of adverse effects can be increased when PRO-542 is combined with Galcanezumab.
TNX-901 The risk or severity of adverse effects can be increased when TNX-901 is combined with Galcanezumab.
Inotuzumab ozogamicin The risk or severity of adverse effects can be increased when Inotuzumab ozogamicin is combined with Galcanezumab.
RI 624 The risk or severity of adverse effects can be increased when RI 624 is combined with Galcanezumab.
Stamulumab The risk or severity of adverse effects can be increased when MYO-029 is combined with Galcanezumab.
CT-011 The risk or severity of adverse effects can be increased when CT-011 is combined with Galcanezumab.
Leronlimab The risk or severity of adverse effects can be increased when Leronlimab is combined with Galcanezumab.
Glembatumumab vedotin The risk or severity of adverse effects can be increased when Glembatumumab vedotin is combined with Galcanezumab.
Olaratumab The risk or severity of adverse effects can be increased when Olaratumab is combined with Galcanezumab.
IPH 2101 The risk or severity of adverse effects can be increased when IPH 2101 is combined with Galcanezumab.
TB-402 The risk or severity of adverse effects can be increased when TB-402 is combined with Galcanezumab.
Caplacizumab The risk or severity of adverse effects can be increased when Caplacizumab is combined with Galcanezumab.
IMC-1C11 The risk or severity of adverse effects can be increased when IMC-1C11 is combined with Galcanezumab.
Eldelumab The risk or severity of adverse effects can be increased when Eldelumab is combined with Galcanezumab.
Lumiliximab The risk or severity of adverse effects can be increased when Lumiliximab is combined with Galcanezumab.

Target Protein

Calcitonin gene-related peptide 1 CALCA
Calcitonin gene-related peptide 2 CALCB

Referensi & Sumber

Artikel (PubMed)
  • PMID: 28409893
    Pellesi L, Guerzoni S, Pini LA: Spotlight on Anti-CGRP Monoclonal Antibodies in Migraine: The Clinical Evidence to Date. Clin Pharmacol Drug Dev. 2017 Nov;6(6):534-547. doi: 10.1002/cpdd.345. Epub 2017 Apr 14.
  • PMID: 29019093
    Benemei S, Cortese F, Labastida-Ramirez A, Marchese F, Pellesi L, Romoli M, Vollesen AL, Lampl C, Ashina M: Triptans and CGRP blockade - impact on the cranial vasculature. J Headache Pain. 2017 Oct 10;18(1):103. doi: 10.1186/s10194-017-0811-5.
  • PMID: 29089894
    Monteith D, Collins EC, Vandermeulen C, Van Hecken A, Raddad E, Scherer JC, Grayzel D, Schuetz TJ, de Hoon J: Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the CGRP Binding Monoclonal Antibody LY2951742 (Galcanezumab) in Healthy Volunteers. Front Pharmacol. 2017 Oct 17;8:740. doi: 10.3389/fphar.2017.00740. eCollection 2017.
  • PMID: 25297013
    Dodick DW, Goadsby PJ, Silberstein SD, Lipton RB, Olesen J, Ashina M, Wilks K, Kudrow D, Kroll R, Kohrman B, Bargar R, Hirman J, Smith J: Safety and efficacy of ALD403, an antibody to calcitonin gene-related peptide, for the prevention of frequent episodic migraine: a randomised, double-blind, placebo-controlled, exploratory phase 2 trial. Lancet Neurol. 2014 Nov;13(11):1100-1107. doi: 10.1016/S1474-4422(14)70209-1. Epub 2014 Oct 5.
  • PMID: 24867844
    Vollbracht S, Rapoport AM: New treatments for headache. Neurol Sci. 2014 May;35 Suppl 1:89-97. doi: 10.1007/s10072-014-1747-z.
  • PMID: 28948500
    Deen M, Correnti E, Kamm K, Kelderman T, Papetti L, Rubio-Beltran E, Vigneri S, Edvinsson L, Maassen Van Den Brink A: Blocking CGRP in migraine patients - a review of pros and cons. J Headache Pain. 2017 Sep 25;18(1):96. doi: 10.1186/s10194-017-0807-1.
  • PMID: 30917684
    Kielbasa W, Helton DL: A new era for migraine: Pharmacokinetic and pharmacodynamic insights into monoclonal antibodies with a focus on galcanezumab, an anti-CGRP antibody. Cephalalgia. 2019 Sep;39(10):1284-1297. doi: 10.1177/0333102419840780. Epub 2019 Mar 27.

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