Peringatan Keamanan

Toxicity information regarding cilgavimab is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects. Symptomatic and supportive measures are recommended.L39411

Cilgavimab

DB16393

biotech approved investigational

Deskripsi

SARS-CoV-2, the causative agent of COVID-19, enters cells via the interaction between the trimeric spike (S) glycoprotein and host cell angiotensin-converting enzyme 2 (ACE2). Blocking the interaction between the receptor-binding domain (RBD) of the S1 subunit and ACE2 inhibits viral host cell entry; animal studies indicate that antibodies capable of blocking this interaction reduce viral load and improve clinical symptoms of infection.A243356, A243361 Cilgavimab (formerly AZD1061) is a recombinant monoclonal antibody produced in Chinese hamster ovary (CHO) cells derived from a neutralizing antibody isolated from a patient with a natural history of SARS-CoV-2 infection and modified through targeted amino acid substitutions to exhibit an extended (~85-day) half-life.A243351, A243356, L39411 As the RBD binding site of cilgavimab does not overlap with that of tixagevimab, the two can be administered to synergistically impair SARS-CoV-2 infection in individuals who may be exposed to the virus.A243351, A243361, L39411

Cilgavimab is not approved for any indication by the FDA. Cilgavimab, in combination with tixagevimab, was issued an FDA emergency use authorization (EUA) on December 9, 2021, for the pre-exposure prophylaxis of COVID-19 in individuals at increased risk for whom vaccination is not recommended. The combination is co-packaged and available under the name EVUSHELD (formerly AZD7442).L39411 EVUSHELD was granted marketing authorization by the EMA on March 28, 2022,L41454 and was approved in Canada soon after, on April 14, 2022.L41549

In October 2022, the FDA and Health Canada released safety alerts regarding the risk of developing COVID-19 when exposed to SARS-CoV-2 variants not neutralized by EVUSHELD. Certain SARS-CoV-2 Omicron subvariants may be associated with resistance to monoclonal antibodies, such as EVUSHELD. The FDA and Health Canada advise healthcare providers to inform patients of this risk.L43772,L43777

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Cilgavimab has a half-life of 82.9 ± 12.3 days.[L39411]
Volume Distribusi Cilgavimab has an apparent volume of distribution of 8.7 ± 2.73 L.[L39411]
Klirens (Clearance) Cilgavimab has an apparent clearance of 0.074 ± 0.028 L/day.[L39411]

Absorpsi

A single 150 mg intramuscular dose of cilgavimab, given concurrently with 150 mg of tixagevimab, resulted in a Cmax geometric mean (%CV) of 15.3 (38.5) ?g/mL in a median Tmax of 14.0 (range 3.1-60) days. The observed geometric mean (%CV) one, 150, or 210 days following dosing was 3.9 (94.4), 5.5 (35.2), and 3.9 (37.1) ?g/mL. This single dose resulted in an AUC0-? of 2133 (31.7) ?g\*day/mL.L39411

Metabolisme

As a monoclonal antibody, cilgavimab is expected to undergo proteolytic degradation.L39411

Rute Eliminasi

Cilgavimab is unlikely to undergo renal excretion.L39411

Interaksi Obat

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

Target Protein

Spike glycoprotein S

Referensi & Sumber

Artikel (PubMed)
  • PMID: 32651581
    Zost SJ, Gilchuk P, Chen RE, Case JB, Reidy JX, Trivette A, Nargi RS, Sutton RE, Suryadevara N, Chen EC, Binshtein E, Shrihari S, Ostrowski M, Chu HY, Didier JE, MacRenaris KW, Jones T, Day S, Myers L, Eun-Hyung Lee F, Nguyen DC, Sanz I, Martinez DR, Rothlauf PW, Bloyet LM, Whelan SPJ, Baric RS, Thackray LB, Diamond MS, Carnahan RH, Crowe JE Jr: Rapid isolation and profiling of a diverse panel of human monoclonal antibodies targeting the SARS-CoV-2 spike protein. Nat Med. 2020 Sep;26(9):1422-1427. doi: 10.1038/s41591-020-0998-x. Epub 2020 Jul 10.
  • PMID: 32668443
    Zost SJ, Gilchuk P, Case JB, Binshtein E, Chen RE, Nkolola JP, Schafer A, Reidy JX, Trivette A, Nargi RS, Sutton RE, Suryadevara N, Martinez DR, Williamson LE, Chen EC, Jones T, Day S, Myers L, Hassan AO, Kafai NM, Winkler ES, Fox JM, Shrihari S, Mueller BK, Meiler J, Chandrashekar A, Mercado NB, Steinhardt JJ, Ren K, Loo YM, Kallewaard NL, McCune BT, Keeler SP, Holtzman MJ, Barouch DH, Gralinski LE, Baric RS, Thackray LB, Diamond MS, Carnahan RH, Crowe JE Jr: Potently neutralizing and protective human antibodies against SARS-CoV-2. Nature. 2020 Aug;584(7821):443-449. doi: 10.1038/s41586-020-2548-6. Epub 2020 Jul 15.
  • PMID: 34548634
    Dong J, Zost SJ, Greaney AJ, Starr TN, Dingens AS, Chen EC, Chen RE, Case JB, Sutton RE, Gilchuk P, Rodriguez J, Armstrong E, Gainza C, Nargi RS, Binshtein E, Xie X, Zhang X, Shi PY, Logue J, Weston S, McGrath ME, Frieman MB, Brady T, Tuffy KM, Bright H, Loo YM, McTamney PM, Esser MT, Carnahan RH, Diamond MS, Bloom JD, Crowe JE Jr: Genetic and structural basis for SARS-CoV-2 variant neutralization by a two-antibody cocktail. Nat Microbiol. 2021 Oct;6(10):1233-1244. doi: 10.1038/s41564-021-00972-2. Epub 2021 Sep 21.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Evusheld
    Injection, solution • - • Intramuscular • EU • Approved
  • Evusheld
    Injection, solution; Kit • - • Intramuscular; Intravenous • US
  • Evusheld
    Solution • - • Intramuscular • Canada • Approved

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