Peringatan Keamanan

LD50 and overdose information are not currently available, but effects of an overdose are likely to impact the lungs, heart, and circulatory system, leading to significant toxicity.L10842

Trastuzumab deruxtecan

DB14962

biotech approved investigational

Deskripsi

Trastuzumab deruxtecan is a HER2-directed antibody attached to a topoisomerase inhibitor that is approved for use in certain types of treatment-resistant HER2-positive cancers.L10842 It is classified as an antibody-drug conjugate. The cleavable peptide linker used to bind the antibody and drug in this product distinguishes it from other members of its class.A188988

Trastuzumab deruxtecan was developed by Daiichi Sankyo in collaboration with AstraZeneca and was first approved by the FDA in 2019.L10842

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) In a pharmacokinetic study, the median elimination half-life of trastuzumab deruxtecan was about 5.8 days.[L10842]
Volume Distribusi The estimated volume of distribution of trastuzumab deruxtecan in the central compartment is 2.77 L, according to a population based pharmacokinetic study.[L10842] Pharmacokinetic studies found that the unchanged drug is distributed in the blood and is not significantly retained in tissues.[A188979]
Klirens (Clearance) Trastuzumab deruxtecan is rapidly cleared from systemic circulation.[A188979] Estimated systemic clearance of trastuzumab deruxtecan is 0.42 L/day, according to a population pharmacokinetic analysis. DXd showed a systemic clearance of about 19.2 L/h.[L10842]

Absorpsi

The Cmax of trastuzumab deruxtecan at normal therapeutic doses was 122 ?g/mL (20%). The AUC of trastuzumab deruxtecan was 735 ?g·day/mL (31%).L10842

Metabolisme

Trastuzumab deruxtecan is likely broken down into small peptides and amino acids through catabolism, just as the metabolism of endogenous IgG.A189009,L10842 Cathepsin B and L enzymes are thought to be involved in the cleavage of the peptide linker that joins the topoisomerase I inhibitor and the antibody.A188988 In vitro, DXd, the topoisomerase inhibitor portion of the drug, is found to be metabolized by CYP3A4.L10842

Rute Eliminasi

A pharmacokinetic study revealed that this drug was mainly excreted in the feces. Another study determined that 67% of a dose was excreted in the feces.A188979,A188988 Unmetabolized DXd was found in the urine during a pharmacokinetic study.A188979

Interaksi Obat

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

Target Protein

High affinity immunoglobulin gamma Fc receptor I FCGR1A
DNA topoisomerase 1 TOP1

Referensi & Sumber

Synthesis reference: Nakada T, Masuda T, Naito H, Yoshida M, Ashida S, Morita K, Miyazaki H, Kasuya Y, Ogitani Y, Yamaguchi J, Abe Y2, Honda T2. (2016).Novel antibody drug conjugates containing exatecan derivative-based cytotoxic payloads. Bioorg Med Chem Lett.,Mar 15;26(6):1542-1545
Artikel (PubMed)
  • PMID: 31047803
    Tamura K, Tsurutani J, Takahashi S, Iwata H, Krop IE, Redfern C, Sagara Y, Doi T, Park H, Murthy RK, Redman RA, Jikoh T, Lee C, Sugihara M, Shahidi J, Yver A, Modi S: Trastuzumab deruxtecan (DS-8201a) in patients with advanced HER2-positive breast cancer previously treated with trastuzumab emtansine: a dose-expansion, phase 1 study. Lancet Oncol. 2019 Jun;20(6):816-826. doi: 10.1016/S1470-2045(19)30097-X. Epub 2019 Apr 29.
  • PMID: 30351177
    Nagai Y, Oitate M, Shiozawa H, Ando O: Comprehensive preclinical pharmacokinetic evaluations of trastuzumab deruxtecan (DS-8201a), a HER2-targeting antibody-drug conjugate, in cynomolgus monkeys. Xenobiotica. 2019 Sep;49(9):1086-1096. doi: 10.1080/00498254.2018.1531158. Epub 2019 Jan 4.
  • PMID: 31825192
    Modi S, Saura C, Yamashita T, Park YH, Kim SB, Tamura K, Andre F, Iwata H, Ito Y, Tsurutani J, Sohn J, Denduluri N, Perrin C, Aogi K, Tokunaga E, Im SA, Lee KS, Hurvitz SA, Cortes J, Lee C, Chen S, Zhang L, Shahidi J, Yver A, Krop I: Trastuzumab Deruxtecan in Previously Treated HER2-Positive Breast Cancer. N Engl J Med. 2019 Dec 11. doi: 10.1056/NEJMoa1914510.
  • PMID: 31563805
    Xu Z, Guo D, Jiang Z, Tong R, Jiang P, Bai L, Chen L, Zhu Y, Guo C, Shi J, Yu D: Novel HER2-Targeting Antibody-Drug Conjugates of Trastuzumab Beyond T-DM1 in Breast Cancer: Trastuzumab Deruxtecan(DS-8201a) and (Vic-)Trastuzumab Duocarmazine (SYD985). Eur J Med Chem. 2019 Dec 1;183:111682. doi: 10.1016/j.ejmech.2019.111682. Epub 2019 Sep 6.
  • PMID: 28367126
    Kendrick F, Evans ND, Arnulf B, Avet-Loiseau H, Decaux O, Dejoie T, Fouquet G, Guidez S, Harel S, Hebraud B, Javaugue V, Richez V, Schraen S, Touzeau C, Moreau P, Leleu X, Harding S, Chappell MJ: Analysis of a Compartmental Model of Endogenous Immunoglobulin G Metabolism with Application to Multiple Myeloma. Front Physiol. 2017 Mar 17;8:149. doi: 10.3389/fphys.2017.00149. eCollection 2017.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Enhertu
    Injection, powder, lyophilized, for solution • 100 mg/5mL • Intravenous • US • Approved
  • Enhertu
    Powder, for solution • 100 mg / vial • Intravenous • Canada • Approved
  • Enhertu
    Injection, powder, for solution • 100 mg • Intravenous • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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