Peringatan Keamanan

There is limited information regarding the acute toxicity profile and overdosage of tremelimumab. The maximum tolerated dose in non-human primates was 100 mg/kg.L43662

Tremelimumab

DB11771

biotech approved investigational

Deskripsi

Tremelimumab, formerly known as ticilimumab, is a fully human IgG2 monoclonal antibody directed against cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4). CTLA-4 is a cell surface receptor expressed on activated T cells to act as a negative regulator for T cells.A253717 By binding to CTLA-4, tremelimumab enhances T cell-mediated killing of tumours and reduces tumour growth.A253717, L43652 Because CTLA-4 is an immune checkpoint that plays a vital role in regulating T cell-mediated immune response, tremelimumab is considered an immune checkpoint inhibitor, which is an emerging cancer immunotherapy drug class.A253712

Tremelimumab was first approved by the FDA in October 2022 to be used in combination with durvalumab to treat hepatocellular carcinoma.L43652 It is also being investigated in other cancers, such as colon cancer, pancreatic cancer, non-small cell lung cancer (NSCLC), and malignant melanoma.A253717, A253722 After receiving an EMA Committee for Medicinal Products for Human Use (CHMP) recommendation in December 2022, tremelimumab was approved for combined use with durvalumab.L46188

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 geometric mean (CV%) terminal half-life of tremelimumab was 16.9 days (19%) after a single dose and 18.2 days (19%) during steady-state.[L43652]
Volume Distribusi The geometric mean (% coefficient of variation [CV%]) of tremelimumab for central (V1) and peripheral (V2) volume of distribution was 3.45 (24%) and 2.66 (34%) L, respectively.[L43652]
Klirens (Clearance) The geometric mean (CV%) clearance of tremelimumab was 0.286 L/day (32%) after a single dose and 0.263 L/day (32%) during steady-state.[L43652]

Absorpsi

In patients with solid tumours who received tremelimumab doses 1 mg/kg, 3 mg/kg, and 10 mg/kg (1- to 10-times the approved recommended dosage) once every four weeks for four doses, the AUC of tremelimumab increased proportionally and steady-state was achieved at approximately 12 weeks.L43652

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

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

Target Protein

Cytotoxic T-lymphocyte protein 4 CTLA4

Referensi & Sumber

Artikel (PubMed)
  • PMID: 23444951
    Tarhini AA: Tremelimumab: a review of development to date in solid tumors. Immunotherapy. 2013 Mar;5(3):215-29. doi: 10.2217/imt.13.9.
  • PMID: 20698721
    Authors unspecified: Tremelimumab. Drugs R D. 2010;10(2):123-32. doi: 10.2165/11584530-000000000-00000.
  • PMID: 34105088
    Arru C, De Miglio MR, Cossu A, Muroni MR, Carru C, Zinellu A, Paliogiannis P: Durvalumab Plus Tremelimumab in Solid Tumors: A Systematic Review. Adv Ther. 2021 Jul;38(7):3674-3693. doi: 10.1007/s12325-021-01796-6. Epub 2021 Jun 8.
  • PMID: 29118008
    Rowshanravan B, Halliday N, Sansom DM: CTLA-4: a moving target in immunotherapy. Blood. 2018 Jan 4;131(1):58-67. doi: 10.1182/blood-2017-06-741033. Epub 2017 Nov 8.
  • PMID: 32439954
    Hwang JR, Byeon Y, Kim D, Park SG: Recent insights of T cell receptor-mediated signaling pathways for T cell activation and development. Exp Mol Med. 2020 May;52(5):750-761. doi: 10.1038/s12276-020-0435-8. Epub 2020 May 21.
  • PMID: 21074059
    Ribas A: Clinical development of the anti-CTLA-4 antibody tremelimumab. Semin Oncol. 2010 Oct;37(5):450-4. doi: 10.1053/j.seminoncol.2010.09.010.
  • PMID: 17673618
    Ribas A, Hanson DC, Noe DA, Millham R, Guyot DJ, Bernstein SH, Canniff PC, Sharma A, Gomez-Navarro J: Tremelimumab (CP-675,206), a cytotoxic T lymphocyte associated antigen 4 blocking monoclonal antibody in clinical development for patients with cancer. Oncologist. 2007 Jul;12(7):873-83. doi: 10.1634/theoncologist.12-7-873.

Contoh Produk & Brand

Produk: 7 • International brands: 0
Produk
  • Imjudo
    Injection, solution, concentrate • 20 mg/ml • Intravenous • EU • Approved
  • Imjudo
    Injection, solution, concentrate • 20 mg/ml • Intravenous • EU • Approved
  • Imjudo
    Injection, solution • 25 mg/1.25mL • Intravenous • US • Approved
  • Imjudo
    Injection, solution • 300 mg/15mL • Intravenous • US • Approved
  • Imjudo
    Solution • 20 mg / mL • Intravenous • Canada • Approved
  • Tremelimumab Astrazeneca
    Injection, solution, concentrate • 20 mg/ml • Intravenous • EU
  • Tremelimumab Astrazeneca
    Injection, solution, concentrate • 20 mg/ml • Intravenous • EU

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