Axatilimab

DB16388

biotech approved investigational

Deskripsi

Axatilimab is a humanized IgG4 monoclonal antibody produced in Chinese hamster ovary cells.L51194 It is targeted against macrophage colony-stimulating factor 1 receptor (CSF-1R), causing a reduction in circulating levels of monocytes and macrophages responsible for the symptoms associated with chronic graft-versus-host disease (cGVHD).L51194 The mainstay of cGVHD treatment are systemic corticosteroids, but they are ineffective in 30-50% of cases.A264309 Approved treatment options in steroid-refractory cGHVD are limited, and include ruxolitinib, ibrutinib, and belumosudil.A264309

Axatilimab was approved by the FDA in August 2024 for the third-line treatment of cGVHD.L51194,L51199 It is the first FDA-approved anti-CSF-1R antibody directed against inflammatory and fibrotic drivers in chronic graft-versus-host disease.L51199

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) The mean terminal half-life of axatilimab-csfr increased from 10.7 hours to 108 hours over a dose range of 0.15 mg/kg to 3 mg/kg.[L51194]
Volume Distribusi The volume of distribution of axatilimab-csfr is 6.06 L.[L51194]
Klirens (Clearance) The total clearance of axatilimab-csfr is 0.07 L/h,[L51194] and is composed of linear and non-linear components such that clearance decreased from 2.32 mL/h/kg to 0.21 mL h/kg following single-dose administrations over a dose range of 0.15 mg/kg to 3 mg/kg.[L51194] The median time to 97% reduction from C<sub>max</sub> after the end of infusion is 4 days at a dose of 0.3 mg/kg.[L51194]

Absorpsi

The AUC of axatilimab-csfr increased in a greater than dose-proportional manner following single-dose administration over a dose range of 0.15 mg/kg to 3 mg/kg in healthy subjects.L51194 Axatilimab-csfr does not appear to accumulate when administered at the approved recommended dosage.L51194

Metabolisme

As with other therapeutic proteins, axatilimab is likely metabolized into smaller peptides and amino acids by catabolic pathways.L51194

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

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

Target Protein

Macrophage colony-stimulating factor 1 receptor CSF1R

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25157821
    Alexander KA, Flynn R, Lineburg KE, Kuns RD, Teal BE, Olver SD, Lor M, Raffelt NC, Koyama M, Leveque L, Le Texier L, Melino M, Markey KA, Varelias A, Engwerda C, Serody JS, Janela B, Ginhoux F, Clouston AD, Blazar BR, Hill GR, MacDonald KP: CSF-1-dependant donor-derived macrophages mediate chronic graft-versus-host disease. J Clin Invest. 2014 Oct;124(10):4266-80. doi: 10.1172/JCI75935. Epub 2014 Aug 26.
  • PMID: 38094101
    Kovalenko I, Saleem T, Shah M, Seyedroudbari S, Golubykh K, Ali R, Mirza T, Laek B, Wahab A, Chattaraj A, Proskuriakova E, Garg C, Khan R: Novel Pharmacological Treatment Options of Steroid-Refractory Graft-versus-Host Disease. Adv Hematol. 2023 Dec 6;2023:9949961. doi: 10.1155/2023/9949961. eCollection 2023.
  • PMID: 36459673
    Kitko CL, Arora M, DeFilipp Z, Zaid MA, Di Stasi A, Radojcic V, Betts CB, Coussens LM, Meyers ML, Qamoos H, Ordentlich P, Kumar V, Quaranto C, Schmitt A, Gu Y, Blazar BR, Wang TP, Salhotra A, Pusic I, Jagasia M, Lee SJ: Axatilimab for Chronic Graft-Versus-Host Disease After Failure of at Least Two Prior Systemic Therapies: Results of a Phase I/II Study. J Clin Oncol. 2023 Apr 1;41(10):1864-1875. doi: 10.1200/JCO.22.00958. Epub 2022 Dec 2.

Contoh Produk & Brand

Produk: 1 • International brands: 0
Produk
  • Niktimvo
    Injection • 50 mg/1mL • Intravenous • US • Approved

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