Peringatan Keamanan

There are no data regarding overdosage with pembrolizumab.

Pembrolizumab

DB09037

biotech approved

Deskripsi

Pembrolizumab is a highly selective IgG4-kappa humanized monoclonal antibody against PD-1 receptors. It was generated by grafting the variable sequences of a very high-affinity mouse antihuman PD-1 antibody onto a human IgG4-kappa isotype containing a stabilizing S228P Fc mutation.A18829 It contains 32 cysteine residues and the complete folded molecule includes 4 disulfide linkages as interchain bonds and 23 interchain bonds.F136 It was developed by Merck & Co and first approved for the treatment of metastatic malignant melanoma by the FDA on September 4, 2014,L2954 becoming the first approved therapy against PD-1.A7624 In the time since its initial approval, pembrolizumab has been granted approval in the treatment of a wide variety of cancers.L38934,L43257

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 terminal half-life of pembrolizumab is 22 days.[L38934]
Volume Distribusi The steady-state volume of distribution of pembrolizumab is approximately 6 liters.[L38934]
Klirens (Clearance) Clearance is moderately lower at steady-state (195 mL/day) than after the first dose (252 mL/day), although this decrease is not clinically significant.[L38934]

Absorpsi

Intravenously administered pembrolizumab is completely bioavailable. Steady-state is reached after approximately 16 weeks.L38934

Metabolisme

Pembrolizumab is catalyzed into smaller peptides and amino acids via general protein degradation.A18829

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

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

Target Protein

Programmed cell death protein 1 PDCD1
Programmed cell death 1 ligand 1 CD274

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25034862
    Robert C, Ribas A, Wolchok JD, Hodi FS, Hamid O, Kefford R, Weber JS, Joshua AM, Hwu WJ, Gangadhar TC, Patnaik A, Dronca R, Zarour H, Joseph RW, Boasberg P, Chmielowski B, Mateus C, Postow MA, Gergich K, Elassaiss-Schaap J, Li XN, Iannone R, Ebbinghaus SW, Kang SP, Daud A: Anti-programmed-death-receptor-1 treatment with pembrolizumab in ipilimumab-refractory advanced melanoma: a randomised dose-comparison cohort of a phase 1 trial. Lancet. 2014 Sep 20;384(9948):1109-17. doi: 10.1016/S0140-6736(14)60958-2. Epub 2014 Jul 15.
  • PMID: 25331768
    Poole RM: Pembrolizumab: first global approval. Drugs. 2014 Oct;74(16):1973-81. doi: 10.1007/s40265-014-0314-5.
  • PMID: 27485741
    Longoria TC, Tewari KS: Evaluation of the pharmacokinetics and metabolism of pembrolizumab in the treatment of melanoma. Expert Opin Drug Metab Toxicol. 2016 Oct;12(10):1247-53. doi: 10.1080/17425255.2016.1216976. Epub 2016 Aug 16.
  • PMID: 26288737
    Khoja L, Butler MO, Kang SP, Ebbinghaus S, Joshua AM: Pembrolizumab. J Immunother Cancer. 2015 Aug 18;3:36. doi: 10.1186/s40425-015-0078-9. eCollection 2015.
  • PMID: 27822406
    Jazirehi AR, Lim A, Dinh T: PD-1 inhibition and treatment of advanced melanoma-role of pembrolizumab. Am J Cancer Res. 2016 Oct 1;6(10):2117-2128. eCollection 2016.

Contoh Produk & Brand

Produk: 6 • International brands: 0
Produk
  • Keytruda
    Injection, powder, lyophilized, for solution • 50 mg/2mL • Intravenous • US • Approved
  • Keytruda
    Injection, solution • 25 mg/1mL • Intravenous • US • Approved
  • Keytruda
    Powder, for solution • 50 mg / vial • Intravenous • Canada • Approved
  • Keytruda
    Solution • 25 mg / mL • Intravenous • Canada • Approved
  • Keytruda
    Injection, powder, for solution • 50 mg • Intravenous • EU • Approved
  • Keytruda
    Injection, solution, concentrate • 25 mg/ml • Intravenous • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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