Trastuzumab deruxtecan
Identification
- Summary
Trastuzumab deruxtecan is an antibody used to treat certain types of unresectable or metastatic HER2 positive breast cancer.
- Brand Names
- Enhertu
- Generic Name
- Trastuzumab deruxtecan
- DrugBank Accession Number
- DB14962
- Background
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.6 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.4
Trastuzumab deruxtecan was developed by Daiichi Sankyo in collaboration with AstraZeneca and was first approved by the FDA in 2019.6
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Chemical Formula
- Not Available
- Protein Average Weight
- Not Available
- Sequences
- Not Available
- Synonyms
- fam-trastuzumab deruxtecan-nxki
- Trastuzumab deruxtecan
- External IDs
- DS-8201
- DS-8201A
- WHO 10516
Pharmacology
- Indication
In the US, trastuzumab deruxtecan is indicated for the treatment of adult patients with unresectable or metastatic HER2-positive breast cancer who have received a prior anti-HER2-based regimen either in the metastatic setting, or in the neoadjuvant or adjuvant setting and have developed disease recurrence during or within six months of completing therapy.6 It is also indicated to treat adults with unresectable or metastatic HER2-low (IHC 1+ or IHC 2+/ISH-) breast cancer who have received a prior chemotherapy in the metastatic setting or developed disease recurrence during or within 6 months of completing adjuvant chemotherapy.6 Trastuzumab deruxtecan is also indicated to treat adult patients with locally advanced or metastatic HER2-positive gastric or gastroesophageal junction adenocarcinoma who have received a prior trastuzumab-based regimen.6
In Canada, trastuzumab deruxtecan is indicated for the treatment of adult patients with unresectable or metastatic HER2-positive breast cancer who have previously been treated with trastuzumab emtansine, or who have received at least one prior anti-HER2-based regimen either in the metastatic setting or in the adjuvant/neoadjuvant setting who have experienced disease recurrence during or within 6 months of adjuvant/neoadjuvant therapy.8 Trastuzumab deruxtecan is also indicated in Canada for the treatment of adult patients with unresectable or metastatic HER2-low breast cancer who have received at least one prior line of chemotherapy in the metastatic setting or developed disease recurrence during or within 6 months of completing adjuvant chemotherapy.8
In Europe, trastuzumab deruxtecan is indicated as monotherapy for the treatment of adult patients with unresectable or metastatic HER2-positive breast cancer who have received one or more prior anti-HER2-based regimens and unresectable or metastatic HER2-low breast cancer who have received prior chemotherapy in the metastatic setting or developed disease recurrence during or within 6 months of completing adjuvant chemotherapy.9 It is also indicated for the treatment of adult patients with advanced HER2-positive gastric or gastroesophageal junction (GEJ) adenocarcinoma who have received a prior trastuzumab-based regimen.9 It is also indicated as a monotherapy for the treatment of adult patients with advanced non-small cell lung cancer whose tumors have an activating HER2 mutation and who require systemic therapy following platinum-based chemotherapy with or without immunotherapy.9
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Advanced gastric adenocarcinoma •••••••••••• ••••• •••••••••• ••••••• •••• ••••••••••• •••••••••• ••••••• •••••••••••• ••• •••••••• Treatment of Advanced gastroesophageal adenocarcinoma •••••••••••• ••••• •••••••••• ••••••• •••• ••••••••••• •••••••••• ••••••• •••••••••••• ••• •••••••• Treatment of Advanced non-small cell lung cancer (nsclc) •••••••••••• ••••• •••••••••• ••••••• •••••••••••• ••• •••••••• Treatment of Metastatic breast cancer •••••••••••• ••••• •••••••••• ••••••• •••••••••••• ••• •••••••• Treatment of Unresectable breast cancer •••••••••••• ••••• •••••••••• ••••••• •••••••••••• ••• •••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Trastuzumab demonstrates antitumor activity against certain types of HER2 positive breast cancer, however, clinical trials are still ongoing to confirm its efficacy.3,6,7 By exploiting both targeted antibody and cytotoxic effects, trastuzumab deruxtecan can effectively destroy tumors.4
The FDA label warns of a potential risk for neutropenia, interstitial lung disease/pneumonitis, and left ventricular dysfunction following the use of this drug.6
- Mechanism of action
Trastuzumab deruxtecan is a humanized anti-HER2 IgG1 antibody, targeting cancer cause by mutation of the HER2 gene. In addition, the small molecule portion of this drug, deruxtecan (DXd), is a topoisomerase I inhibitor.1,6 It is attached to the antibody by a peptide linker. After trastuzumab deruxtecan binds to HER2 found on malignant cells, it is internalized and linker cleavage occurs through the actions of lysosomal enzymes. After it is released through cleavage, DXd causes targeted DNA damage and apoptosis in cancer cells, due to the ability to cross cell membranes.4,6
Normally, drugs in this class (antibody-drug conjugates) present a challenge. The monoclonal antibody accurately targets cancer cells, however exert limited killing action. The addition of a cytotoxic agent (a topoisomerase I inhibitor in this case) effectively kills dividing cancer cells, including those in the healthy tissues, leading to various adverse effects. The peptide linker used to formulate this drug is cleavable, which is unique to other antibody-drug conjugates, allowing for increased efficacy and reduced drug resistance to topoisomerase.4
Target Actions Organism AHigh affinity immunoglobulin gamma Fc receptor I antibodyHumans ADNA topoisomerase 1 inhibitorHumans - Absorption
The Cmax of trastuzumab deruxtecan at normal therapeutic doses was 122 μg/mL (20%). The AUC of trastuzumab deruxtecan was 735 μg·day/mL (31%).6
- Volume of distribution
The estimated volume of distribution of trastuzumab deruxtecan in the central compartment is 2.77 L, according to a population based pharmacokinetic study.6 Pharmacokinetic studies found that the unchanged drug is distributed in the blood and is not significantly retained in tissues.2
- Protein binding
The Dxd portion of the drug has a plasma protein binding estimated at 97%.6
- Metabolism
Trastuzumab deruxtecan is likely broken down into small peptides and amino acids through catabolism, just as the metabolism of endogenous IgG.5,6 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.4 In vitro, DXd, the topoisomerase inhibitor portion of the drug, is found to be metabolized by CYP3A4.6
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- Route of elimination
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.2,4 Unmetabolized DXd was found in the urine during a pharmacokinetic study.2
- Half-life
In a pharmacokinetic study, the median elimination half-life of trastuzumab deruxtecan was about 5.8 days.6
- Clearance
Trastuzumab deruxtecan is rapidly cleared from systemic circulation.2 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.6
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
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.6
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Trastuzumab deruxtecan. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Trastuzumab deruxtecan. Aducanumab The risk or severity of adverse effects can be increased when Aducanumab is combined with Trastuzumab deruxtecan. Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Trastuzumab deruxtecan. Alirocumab The risk or severity of adverse effects can be increased when Alirocumab is combined with Trastuzumab deruxtecan. - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Enhertu Powder, for solution 100 mg / vial Intravenous Astra Zeneca 2021-07-09 Not applicable Canada Enhertu Injection, powder, lyophilized, for solution 100 mg/5mL Intravenous Daiichi Sankyo Inc. 2019-12-20 Not applicable US Enhertu Injection, powder, for solution 100 mg Intravenous Daiichi Sankyo Europe, Gmb H 2021-03-03 Not applicable EU
Categories
- ATC Codes
- L01FD04 — Trastuzumab deruxtecan
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Antibody-drug Conjugates
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- BCRP/ABCG2 Substrates
- Blood Proteins
- Cancer immunotherapy
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Globulins
- HER2 (Human Epidermal Growth Factor Receptor 2) inhibitors
- HER2 Receptor Antagonists
- Immunoglobulins
- Immunologic Factors
- Immunoproteins
- Immunotherapy
- MATE 2 Substrates
- MATE substrates
- MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
- Noxae
- OATP1B3 substrates
- P-glycoprotein substrates
- Proteins
- Serum Globulins
- Topoisomerase Inhibitors
- Toxic Actions
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 5384HK7574
- CAS number
- 1826843-81-5
References
- 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
- General References
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- FDA Approved Drug Products: Enhertu (fam-trastuzumab deruxtecan-nxki) for injection, for intravenous use [Link]
- FDA approves new treatment option for patients with HER2-positive breast cancer who have progressed on available therapies [Link]
- Health Canada Approved Drug Products: Enhertu (trastuzumab deruxtecan) powder for concentrate for intravenous infusion [Link]
- EMA Approved Drug Products: Enhertu (Trastuzumab deruxtecan) Powder for concentrate for solution for infusion. [Link]
- External Links
- 2267574
- Wikipedia
- Trastuzumab_deruxtecan
- FDA label
- Download (590 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Not Yet Recruiting Treatment Breast Cancer 1 4 Recruiting Diagnostic Anatomic Stage IV Breast Cancer AJCC v8 / Brain Metastases / Metastatic Breast Carcinoma 1 3 Active Not Recruiting Treatment Advanced or Metastatic Breast Cancer 1 3 Active Not Recruiting Treatment Breast Cancer 4 3 Active Not Recruiting Treatment HER2-Positive Primary Breast Cancer / Residual Invasive Breast Cancer 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, for solution Intravenous 100 MG Injection, powder, lyophilized, for solution Intravenous 100 mg/5mL Powder, for solution Intravenous 100 mg / vial Solution Intravenous 100 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Not Available
- Experimental Properties
- Not Available
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antibody
- General Function
- Receptor signaling protein activity
- Specific Function
- High affinity receptor for the Fc region of immunoglobulins gamma. Functions in both innate and adaptive immune responses.
- Gene Name
- FCGR1A
- Uniprot ID
- P12314
- Uniprot Name
- High affinity immunoglobulin gamma Fc receptor I
- Molecular Weight
- 42631.525 Da
References
- 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. [Article]
- 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. [Article]
- FDA Approved Drug Products: Enhertu (fam-trastuzumab deruxtecan-nxki) for injection, for intravenous use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Poly(a) rna binding
- Specific Function
- Releases the supercoiling and torsional tension of DNA introduced during the DNA replication and transcription by transiently cleaving and rejoining one strand of the DNA duplex. Introduces a singl...
- Gene Name
- TOP1
- Uniprot ID
- P11387
- Uniprot Name
- DNA topoisomerase 1
- Molecular Weight
- 90725.19 Da
References
- 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. [Article]
- FDA Approved Drug Products: Enhertu (fam-trastuzumab deruxtecan-nxki) for injection, for intravenous use [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- Curator comments
- Lysosomal glucosidase is a popular lysosomal enzyme and likely participates in the breakdown of this drug, but other lysosomal enzymes also contribute.
- General Function
- Maltose alpha-glucosidase activity
- Specific Function
- Essential for the degradation of glygogen to glucose in lysosomes.
- Gene Name
- GAA
- Uniprot ID
- P10253
- Uniprot Name
- Lysosomal alpha-glucosidase
- Molecular Weight
- 105322.935 Da
References
- 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. [Article]
- Wolska-Washer A, Robak T: Safety and Tolerability of Antibody-Drug Conjugates in Cancer. Drug Saf. 2019 Feb;42(2):295-314. doi: 10.1007/s40264-018-0775-7. [Article]
- Pernas S, Tolaney SM: HER2-positive breast cancer: new therapeutic frontiers and overcoming resistance. Ther Adv Med Oncol. 2019 Mar 19;11:1758835919833519. doi: 10.1177/1758835919833519. eCollection 2019. [Article]
- Rinnerthaler G, Gampenrieder SP, Greil R: HER2 Directed Antibody-Drug-Conjugates beyond T-DM1 in Breast Cancer. Int J Mol Sci. 2019 Mar 5;20(5). pii: ijms20051115. doi: 10.3390/ijms20051115. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Poly(a) rna binding
- Specific Function
- Releases the supercoiling and torsional tension of DNA introduced during the DNA replication and transcription by transiently cleaving and rejoining one strand of the DNA duplex. Introduces a singl...
- Gene Name
- TOP1
- Uniprot ID
- P11387
- Uniprot Name
- DNA topoisomerase 1
- Molecular Weight
- 90725.19 Da
References
- 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. [Article]
- Wolska-Washer A, Robak T: Safety and Tolerability of Antibody-Drug Conjugates in Cancer. Drug Saf. 2019 Feb;42(2):295-314. doi: 10.1007/s40264-018-0775-7. [Article]
- Pernas S, Tolaney SM: HER2-positive breast cancer: new therapeutic frontiers and overcoming resistance. Ther Adv Med Oncol. 2019 Mar 19;11:1758835919833519. doi: 10.1177/1758835919833519. eCollection 2019. [Article]
- FDA Approved Drug Products: Enhertu (fam-trastuzumab deruxtecan-nxki) for injection, for intravenous use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Proteoglycan binding
- Specific Function
- Thiol protease which is believed to participate in intracellular degradation and turnover of proteins. Has also been implicated in tumor invasion and metastasis.
- Gene Name
- CTSB
- Uniprot ID
- P07858
- Uniprot Name
- Cathepsin B
- Molecular Weight
- 37821.35 Da
References
- 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. [Article]
- Rinnerthaler G, Gampenrieder SP, Greil R: HER2 Directed Antibody-Drug-Conjugates beyond T-DM1 in Breast Cancer. Int J Mol Sci. 2019 Mar 5;20(5). pii: ijms20051115. doi: 10.3390/ijms20051115. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Serpin family protein binding
- Specific Function
- Important for the overall degradation of proteins in lysosomes.
- Gene Name
- CTSL
- Uniprot ID
- P07711
- Uniprot Name
- Cathepsin L1
- Molecular Weight
- 37563.97 Da
References
- 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. [Article]
- Rinnerthaler G, Gampenrieder SP, Greil R: HER2 Directed Antibody-Drug-Conjugates beyond T-DM1 in Breast Cancer. Int J Mol Sci. 2019 Mar 5;20(5). pii: ijms20051115. doi: 10.3390/ijms20051115. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- 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. [Article]
- FDA Approved Drug Products: Enhertu (fam-trastuzumab deruxtecan-nxki) for injection, for intravenous use [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- 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. [Article]
- FDA Approved Drug Products: Enhertu (fam-trastuzumab deruxtecan-nxki) for injection, for intravenous use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
- Gene Name
- SLCO1B1
- Uniprot ID
- Q9Y6L6
- Uniprot Name
- Solute carrier organic anion transporter family member 1B1
- Molecular Weight
- 76447.99 Da
References
- FDA Approved Drug Products: Enhertu (fam-trastuzumab deruxtecan-nxki) for injection, for intravenous use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
- Gene Name
- SLCO1B3
- Uniprot ID
- Q9NPD5
- Uniprot Name
- Solute carrier organic anion transporter family member 1B3
- Molecular Weight
- 77402.175 Da
References
- FDA Approved Drug Products: Enhertu (fam-trastuzumab deruxtecan-nxki) for injection, for intravenous use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Drug transmembrane transporter activity
- Specific Function
- Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide, metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfate, acy...
- Gene Name
- SLC47A2
- Uniprot ID
- Q86VL8
- Uniprot Name
- Multidrug and toxin extrusion protein 2
- Molecular Weight
- 65083.915 Da
References
- FDA Approved Drug Products: Enhertu (fam-trastuzumab deruxtecan-nxki) for injection, for intravenous use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Transporter activity
- Specific Function
- Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotre...
- Gene Name
- ABCC1
- Uniprot ID
- P33527
- Uniprot Name
- Multidrug resistance-associated protein 1
- Molecular Weight
- 171589.5 Da
References
- FDA Approved Drug Products: Enhertu (fam-trastuzumab deruxtecan-nxki) for injection, for intravenous use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
- Gene Name
- ABCG2
- Uniprot ID
- Q9UNQ0
- Uniprot Name
- ATP-binding cassette sub-family G member 2
- Molecular Weight
- 72313.47 Da
References
- FDA Approved Drug Products: Enhertu (fam-trastuzumab deruxtecan-nxki) for injection, for intravenous use [Link]
Drug created at May 20, 2019 14:38 / Updated at December 22, 2023 19:51