Trastuzumab deruxtecan
Identification
- Summary
Trastuzumab deruxtecan is an antibody used to treat certain types of unresectable or metastatic HER-2 positive breast cancer.
- Brand Names
- Enhertu
- Generic Name
- Trastuzumab deruxtecan
- DrugBank Accession Number
- DB14962
- Background
Trastuzumab deruxtecan is a HER-2 directed antibody attached to a topoisomerase inhibitor that is approved for use in certain types of metastatic, unresectable breast cancer.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 has been granted FDA approval for specific patients with HER-2 positive breast cancer who have failed other treatments.6
Promising results from a clinical trial prompted accelerated FDA approval for this indication on December 20, 2019.7 Trastuzumab deruxtecan was developed by Daiichi Sankyo in collaboration with AstraZeneca. The continued approval of this drug will depend on the confirmation of its beneficial effects in ongoing clinical trials.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
Trastuzumab deruxtecan is indicated for the treatment of adult patients with HER-2 positive breast cancer that is unresectable or metastatic and was previously treated with at least 2 anti-HER2-based regimens while the cancer was metastatic.6
Continued approval will depend on the results of clinical trial results confirming its clinical benefit.6
Accelerate your drug discovery research with the industry’s only fully connected ADMET dataset, ideal for:Accelerate your drug discovery research with our fully connected ADMET dataset- Associated Conditions
- Contraindications & Blackbox Warnings
Contraindications & Blackbox WarningsWith our commercial data, access important information on dangerous risks, contraindications, and adverse effects.Our Blackbox Warnings cover Risks, Contraindications, and Adverse Effects- 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
Hover over products below to view reaction partners
- 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
Reduce medical errorsand improve treatment outcomes with our comprehensive & structured data on drug adverse effects.Reduce medical errors & improve treatment outcomes with our 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
- Not Available
Interactions
- Drug Interactions
- 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. 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. Ansuvimab The risk or severity of adverse effects can be increased when Trastuzumab deruxtecan is combined with Ansuvimab. Anthrax immune globulin human The risk or severity of adverse effects can be increased when Anthrax immune globulin human is combined with Trastuzumab deruxtecan. Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Antilymphocyte immunoglobulin (horse) 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. Asfotase alfa The risk or severity of adverse effects can be increased when Asfotase alfa is combined with Trastuzumab deruxtecan. Atezolizumab The risk or severity of adverse effects can be increased when Atezolizumab is combined with Trastuzumab deruxtecan. 
Improve patient outcomesBuild effective decision support tools with the industry’s most comprehensive drug-drug interaction checker.Learn more - Food Interactions
- No interactions found.
Products
Comprehensive & structured drug product infoFrom application numbers to product codes, connect different identifiers through our commercial datasets.Easily connect various identifiers back to our datasets- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Enhertu Injection, powder, for solution Intravenous Daiichi Sankyo Europe, Gmb H 2021-03-03 Not applicable EU 
Enhertu Injection, powder, lyophilized, for solution 100 mg/5mL Intravenous Daiichi Sankyo Inc. 2019-12-20 Not applicable US 
Enhertu Powder, for solution 100 mg Intravenous Astra Zeneca Not applicable Not applicable Canada 
Categories
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- BCRP/ABCG2 Substrates
- Blood Proteins
- Cancer immunotherapy
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Globulins
- Immunoglobulins
- Immunoproteins
- Immunotherapy
- MATE 2 Substrates
- MATE substrates
- Noxae
- OATP1B3 substrates
- P-glycoprotein substrates
- Proteins
- Serum Globulins
- 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. [PubMed:31047803]
- 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. [PubMed:30351177]
- 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. [PubMed:31825192]
- 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. [PubMed:31563805]
- 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. [PubMed:28367126]
- 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]
- External Links
- 2267574
- Wikipedia
- Trastuzumab_deruxtecan
- FDA label
- Download (590 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Not Yet Recruiting Treatment Breast Cancer 1 3 Active Not Recruiting Treatment Breast Cancer 3 3 Not Yet Recruiting Treatment Adenocarcinomas of the Gastroesophageal Junction / Gastric Cancer, Adenocarcinoma 1 3 Not Yet Recruiting Treatment Breast Cancer; HER2-positive; Metastatic 1 3 Recruiting Treatment Advanced or Metastatic Breast Cancer 1 3 Recruiting Treatment HER2-Positive Primary Breast Cancer / Residual Invasive Breast Cancer 1 2 Active Not Recruiting Treatment Adenocarcinoma - GEJ / Adenocarcinoma Gastric Stage IV With Metastases 1 2 Active Not Recruiting Treatment Breast Cancer 1 2 Active Not Recruiting Treatment Non-Small Cell Lung Carcinoma (NSCLC) 1 2 Active Not Recruiting Treatment Tumors, Breast 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, for solution Intravenous Injection, powder, lyophilized, for solution Intravenous 100 mg/5mL Powder, for solution Intravenous 100 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Not Available
- Experimental Properties
- Not Available
Targets
Accelerate your drug discovery research
with our fully connected ADMET & drug target dataset.
Accelerate your drug discovery research with our ADMET & drug target dataset
- 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. [PubMed:31047803]
- 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. [PubMed:30351177]
- 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. [PubMed:31047803]
- 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. [PubMed:31563805]
- 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. [PubMed:30649747]
- 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. [PubMed:30911337]
- 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. [PubMed:30841523]
- 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. [PubMed:31563805]
- 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. [PubMed:30649747]
- 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. [PubMed:30911337]
- 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. [PubMed:31563805]
- 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. [PubMed:30841523]
- 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. [PubMed:31563805]
- 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. [PubMed:30841523]
- 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. [PubMed:31563805]
- FDA Approved Drug Products: ENHERTU (fam-trastuzumab deruxtecan-nxki) for injection, for intravenous use [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- 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. [PubMed:30351177]
- 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 on May 20, 2019 14:38 / Updated on February 21, 2021 18:55