Identification
- Summary
Estetrol is an estrogen used in combination with drospirenone for oral contraception.
- Brand Names
- Nextstellis 28 Day
- Generic Name
- Estetrol
- DrugBank Accession Number
- DB12235
- Background
Naturally or synthetically produced steroid estrogens have a wide range of pharmaceutical uses ranging from hormonal contraception to the treatment of menopausal symptoms.15 Estetrol (E4) is a native estrogen occurring naturally during pregnancy, but can be synthesized from a plant source and used for contraception.14 It is more potent and is safer than the synthetic estrogen ethinylestradiol (EE2) found in 97% of oral contraceptive pills, reducing the environmental accumulation of unwanted endocrine disrupting chemicals (EDCs) that often lead to harmful epigenetic effects.15
On April 15 2021, Mayne Pharma Group Limited and Mithra Pharmaceuticals were granted FDA approval for the oral contraceptive Estelle/Nextstellis, a combination of drospirenone and estetrol. Estetrol is the first new estrogen introduced to the USA in over 50 years and is the first approved estetrol product in the world. The combination of drospirenone and estetrol offers a new choice with a favourable safety profile for women seeking contraceptive therapy.14 In Canada, Nextstellis was approved for use in March 2021; it was developed by Mithra and is marketed by Searchlight Pharma.18
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Estetrol (DB12235)
- Weight
- Average: 304.3808
Monoisotopic: 304.167459256 - Chemical Formula
- C18H24O4
- Synonyms
- 15α-hydroxyestriol
- Estetrol
- Estétrol
- Estetrolum
- Oestetrol
Pharmacology
- Indication
Estetrol is indicated in combination with drospirenone for the prevention of pregnancy.13
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 Therapies
- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
- Mechanism of action
Estetrol is a synthetic analogue of a naturally occurring estrogen present during pregnancy, demonstrating selectivity for both estrogen receptor-α (ER-α) and ER-β and suppressing ovulation.13 Estetrol binds with a low to moderate affinity human estrogen receptor alpha (ER alpha) and ER beta with a preference for ER alpha.8 Estetrol demonstrates a unique mechanism of action via tissue selective activity, showing estrogen receptor agonist activity on the vagina, the uterus and the endometrium, and negative estrogenic activity on breast tissue.12,18
Target Actions Organism UEstrogen receptor alpha agonistmodulatorregulatorHumans UEstrogen receptor beta agonistHumans - Absorption
Estetrol is rapidly absorbed from the gastrointestinal tract. The Cmax of estetrol is 18 ng/mL according to the results of a pharmacokinetic study, with an AUC of 36.4 ng•h/mL. When estetrol and drospirenone are taken in a single product, maximum serum concentrations of approximately 48.7 ng/mL are achieved within 1-3 h. Bioavailability of the combination ranges between 76 and 85%.17 The Tmax can range from 0.5 to 2 hours and time to steady state is approximately 4 days, according to the results of one clinical study.13
- Volume of distribution
Limited distribution of estetrol into red blood cells has been demonstrated.17
- Protein binding
Estetrol is 46-50% bound to plasma proteins.13 Estetrol does not bind to Sex Hormone Binding Globulin (SHBG). In one study, estetrol showed moderate binding to human plasma proteins (45.5%-50.4%) and human serum albumin (58.6%) with low binding to human alpha-glycoprotein (11.2%).17
- Metabolism
Estretol is heavily metabolized after oral administration.17 Phase 2 metabolism of estrogen forms glucuronide and sulfate conjugates with negligible in-vitro estrogenic activity. In vitro metabolism studies demonstrate that UGT2B7 catalyzes the formation of E4-16-glucuronide. Estetrol is combined with drospirenone in a product. The hepatic cytochrome enzyme CYP3A4 metabolizes drospirenone to two primary metabolites: the acid form of drospirenone through the opening of the lactone ring and the 4,5 dihydrodrospirenone formed by reduction, followed by sulfation. Both metabolites are pharmacologically inactive.13,17
- Route of elimination
Estrogens are generally excreted as sulfated and glucuronidated derivatives.11 Approximately 69% of a dose of estetrol is excreted in the urine, and about 22% is excreted in the feces as unchanged drug.13
- Half-life
The elimination half-life of estetrol is approximately 27 hours.13 Half-life may range between 19-40 hours.7
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
LD50 information for estetrol is not readily available in the literature. Subjects receiving a dose of 20 mg, 40 mg or 60 mg of estetrol per day over 12 weeks were tolerated without dose-limiting toxicity.10 Symptoms that may occur in association with overdose, based on existing information on overdosage with oral contraceptives include nausea, vomiting, and vaginal bleeding. In one clinical study, 1 of 32 healthy research subjects receiving a dose of 75 mg of estretol with 15 mg of drospirenone for 10 days experienced deep vein thrombosis of the lower right limb. There is no known antidote to an estretol overdose; conduct laboratory testing for electrolytes and evidence of metabolic acidosis and provide symptomatic treatment.17
- 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 softwareAbametapir The serum concentration of Estetrol can be increased when it is combined with Abametapir. Abatacept The metabolism of Estetrol can be increased when combined with Abatacept. Abciximab The risk or severity of adverse effects can be increased when Estetrol is combined with Abciximab. Abemaciclib The metabolism of Abemaciclib can be decreased when combined with Estetrol. Acalabrutinib The metabolism of Acalabrutinib can be decreased when combined with Estetrol. Acarbose The therapeutic efficacy of Acarbose can be decreased when used in combination with Estetrol. Acebutolol The risk or severity of hyperkalemia can be increased when Acebutolol is combined with Estetrol. Aceclofenac The risk or severity of hyperkalemia can be increased when Aceclofenac is combined with Estetrol. Acemetacin The risk or severity of hyperkalemia can be increased when Acemetacin is combined with Estetrol. Acenocoumarol The risk or severity of adverse effects can be increased when Estetrol is combined with Acenocoumarol. 
Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- Take with or without food. Take at the same time each day.
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.- Product Ingredients
Ingredient UNII CAS InChI Key Estetrol monohydrate KC3GI9UM9V 2055649-81-3 XRJNAPXFAXBPAM-BVTDNVAGSA-N - International/Other Brands
- Donesta
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Drovelis Estetrol monohydrate (14.2 mg) + Drospirenone (3 mg) Tablet, film coated Oral Gedeon Richter Plc. 2021-10-12 Not applicable EU 
Drovelis Estetrol monohydrate (14.2 mg) + Drospirenone (3 mg) Tablet, film coated Oral Gedeon Richter Plc. 2021-10-12 Not applicable EU Drovelis Estetrol monohydrate (14.2 mg) + Drospirenone (3 mg) Tablet, film coated Oral Gedeon Richter Plc. 2021-10-12 Not applicable EU Drovelis Estetrol monohydrate (14.2 mg) + Drospirenone (3 mg) Tablet, film coated Oral Gedeon Richter Plc. 2021-10-12 Not applicable EU Lydisilka Estetrol monohydrate (14.2 mg) + Drospirenone (3 mg) Tablet, film coated Oral Estetra Sprl 2021-10-15 Not applicable EU Lydisilka Estetrol monohydrate (14.2 mg) + Drospirenone (3 mg) Tablet, film coated Oral Estetra Sprl 2021-10-15 Not applicable EU Lydisilka Estetrol monohydrate (14.2 mg) + Drospirenone (3 mg) Tablet, film coated Oral Estetra Sprl 2021-10-15 Not applicable EU Lydisilka Estetrol monohydrate (14.2 mg) + Drospirenone (3 mg) Tablet, film coated Oral Estetra Sprl 2021-10-15 Not applicable EU Nextstellis Estetrol monohydrate (15 mg) + Drospirenone (3 mg) Tablet Oral Searchlight Pharma Inc 2021-06-15 Not applicable Canada 
Nextstellis Estetrol monohydrate (14.2 mg/1) + Drospirenone (3 mg/1) Kit; Tablet, film coated Oral Mayne Pharma 2021-04-16 Not applicable US 
Categories
- ATC Codes
- G03AA18 — Drospirenone and estetrol
- Drug Categories
- Adrenal Cortex Hormones
- Contraceptives, Oral
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates (strength unknown)
- Cytochrome P-450 Substrates
- Estradiol Congeners
- Estranes
- Estrenes
- Estrogen Contraceptives
- Estrogens
- Estrogens, agonists
- Fused-Ring Compounds
- Genito Urinary System and Sex Hormones
- Gonadal Hormones
- Gonadal Steroid Hormones
- Hormonal Contraceptives for Systemic Use
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Sex Hormones and Modulators of the Genital System
- Steroids
- UGT2B7 substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as estrogens and derivatives. These are steroids with a structure containing a 3-hydroxylated estrane.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Steroids and steroid derivatives
- Sub Class
- Estrane steroids
- Direct Parent
- Estrogens and derivatives
- Alternative Parents
- 3-hydroxysteroids / 17-hydroxysteroids / 16-alpha-hydroxysteroids / Phenanthrenes and derivatives / Tetralins / 1-hydroxy-2-unsubstituted benzenoids / Secondary alcohols / Cyclic alcohols and derivatives / Polyols / Hydrocarbon derivatives
- Substituents
- 1-hydroxy-2-unsubstituted benzenoid / 15-hydroxysteroid / 16-alpha-hydroxysteroid / 16-hydroxysteroid / 17-hydroxysteroid / 3-hydroxysteroid / Alcohol / Aromatic homopolycyclic compound / Benzenoid / Cyclic alcohol
- Molecular Framework
- Aromatic homopolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- ENB39R14VF
- CAS number
- 15183-37-6
- InChI Key
- AJIPIJNNOJSSQC-NYLIRDPKSA-N
- InChI
- InChI=1S/C18H24O4/c1-18-7-6-12-11-5-3-10(19)8-9(11)2-4-13(12)14(18)15(20)16(21)17(18)22/h3,5,8,12-17,19-22H,2,4,6-7H2,1H3/t12-,13-,14-,15-,16-,17+,18+/m1/s1
- IUPAC Name
- (1R,2R,3R,3aS,3bR,9bS,11aS)-11a-methyl-1H,2H,3H,3aH,3bH,4H,5H,9bH,10H,11H,11aH-cyclopenta[a]phenanthrene-1,2,3,7-tetrol
- SMILES
- [H][C@@]12[C@@H](O)[C@@H](O)[C@H](O)[C@@]1(C)CC[C@]1([H])C3=CC=C(O)C=C3CC[C@@]21[H]
References
- Synthesis Reference
Johannes Jan Platteeuw, Herman Jan Tijmen, Coelingh Bennink, Franciscus Wilhelmus, Petrus Damen, Michiel Christian, Alexander Van Vliet. (2013).Process for the preparation of estetrol. (WO2013012328A1).https://patents.google.com/patent/WO2013012328A1/en18
- General References
- Apter D, Zimmerman Y, Beekman L, Mawet M, Maillard C, Foidart JM, Coelingh Bennink HJT: Estetrol combined with drospirenone: an oral contraceptive with high acceptability, user satisfaction, well-being and favourable body weight control. Eur J Contracept Reprod Health Care. 2017 Aug;22(4):260-267. doi: 10.1080/13625187.2017.1336532. Epub 2017 Jun 22. [Article]
- Montt-Guevara MM, Giretti MS, Russo E, Giannini A, Mannella P, Genazzani AR, Genazzani AD, Simoncini T: Estetrol Modulates Endothelial Nitric Oxide Synthesis in Human Endothelial Cells. Front Endocrinol (Lausanne). 2015 Jul 22;6:111. doi: 10.3389/fendo.2015.00111. eCollection 2015. [Article]
- Gaspard U, Taziaux M, Mawet M, Jost M, Gordenne V, Coelingh Bennink HJT, Lobo RA, Utian WH, Foidart JM: A multicenter, randomized study to select the minimum effective dose of estetrol (E4) in postmenopausal women (E4Relief): part 1. Vasomotor symptoms and overall safety. Menopause. 2020 Aug;27(8):848-857. doi: 10.1097/GME.0000000000001561. [Article]
- Abot A, Fontaine C, Buscato M, Solinhac R, Flouriot G, Fabre A, Drougard A, Rajan S, Laine M, Milon A, Muller I, Henrion D, Adlanmerini M, Valera MC, Gompel A, Gerard C, Pequeux C, Mestdagt M, Raymond-Letron I, Knauf C, Ferriere F, Valet P, Gourdy P, Katzenellenbogen BS, Katzenellenbogen JA, Lenfant F, Greene GL, Foidart JM, Arnal JF: The uterine and vascular actions of estetrol delineate a distinctive profile of estrogen receptor alpha modulation, uncoupling nuclear and membrane activation. EMBO Mol Med. 2014 Oct;6(10):1328-46. doi: 10.15252/emmm.201404112. [Article]
- Grandi G, Del Savio MC, Lopes da Silva-Filho A, Facchinetti F: Estetrol (E4): the new estrogenic component of combined oral contraceptives. Expert Rev Clin Pharmacol. 2020 Apr;13(4):327-330. doi: 10.1080/17512433.2020.1750365. Epub 2020 Apr 7. [Article]
- Coelingh Bennink HJT, Verhoeven C, Zimmerman Y, Visser M, Foidart JM, Gemzell-Danielsson K: Pharmacokinetics of the fetal estrogen estetrol in a multiple-rising-dose study in postmenopausal women. Climacteric. 2017 Jun;20(3):285-289. doi: 10.1080/13697137.2017.1291608. Epub 2017 Mar 7. [Article]
- Visser M, Holinka CF, Coelingh Bennink HJ: First human exposure to exogenous single-dose oral estetrol in early postmenopausal women. Climacteric. 2008;11 Suppl 1:31-40. doi: 10.1080/13697130802056511. [Article]
- Visser M, Foidart JM, Coelingh Bennink HJ: In vitro effects of estetrol on receptor binding, drug targets and human liver cell metabolism. Climacteric. 2008;11 Suppl 1:64-8. doi: 10.1080/13697130802050340. [Article]
- Duijkers IJ, Klipping C, Zimmerman Y, Appels N, Jost M, Maillard C, Mawet M, Foidart JM, Coelingh Bennink HJ: Inhibition of ovulation by administration of estetrol in combination with drospirenone or levonorgestrel: Results of a phase II dose-finding pilot study. Eur J Contracept Reprod Health Care. 2015;20(6):476-89. doi: 10.3109/13625187.2015.1074675. [Article]
- Schmidt M, Lenhard H, Hoenig A, Zimmerman Y, Krijgh J, Jansen M, Coelingh Bennink HJT: Tumor suppression, dose-limiting toxicity and wellbeing with the fetal estrogen estetrol in patients with advanced breast cancer. J Cancer Res Clin Oncol. 2020 Nov 26. pii: 10.1007/s00432-020-03472-8. doi: 10.1007/s00432-020-03472-8. [Article]
- Thomas MP, Potter BV: The structural biology of oestrogen metabolism. J Steroid Biochem Mol Biol. 2013 Sep;137:27-49. doi: 10.1016/j.jsbmb.2012.12.014. Epub 2013 Jan 4. [Article]
- Singer CF, Bennink HJ, Natter C, Steurer S, Rudas M, Moinfar F, Appels N, Visser M, Kubista E: Antiestrogenic effects of the fetal estrogen estetrol in women with estrogen-receptor positive early breast cancer. Carcinogenesis. 2014 Nov;35(11):2447-51. doi: 10.1093/carcin/bgu144. Epub 2014 Jul 5. [Article]
- FDA Approved Drug Products: NEXTSTELLIS (drospirenone and estetrol) tablets for oral use [Link]
- Joint press release, Mayne Pharma and Mithra: MAYNE PHARMA AND MITHRA ANNOUNCE FDA APPROVAL OF NEW ORAL CONTRACEPTIVE NEXTSTELLIS [Link]
- Mithra Women's Health: E4 Paves the Road Towards a Revolutionary Era of Environmental Friendly Medicines [Link]
- Cayman Chem MSDS: Estetrol hydrate [Link]
- Product monograph: Nexstellis (estetrol and drospirenone) oral tablets [Link]
- Newswire: Mithra and Searchlight Pharma Announce Nextstellis® Approval in Canada [Link]
- External Links
- PubChem Compound
- 27125
- PubChem Substance
- 347828514
- ChemSpider
- 25245
- BindingDB
- 158505
- 2539031
- ChEBI
- 142773
- ChEMBL
- CHEMBL1230314
- ZINC
- ZINC000005764481
- PDBe Ligand
- 4OH
- Wikipedia
- Estetrol
- PDB Entries
- 3l03
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 3 Active Not Recruiting Prevention Safety 1 3 Completed Prevention Contraception 2 3 Completed Treatment Menopausal Symptoms / Vasomotor Symptoms Associated With Menopause 1 3 Recruiting Treatment Menopausal Symptoms / Vasomotor Symptoms Associated With Menopause 1 2 Active Not Recruiting Treatment Coronavirus Disease 2019 (COVID‑19) 1 2 Completed Prevention Contraception 1 2 Completed Treatment Breast Cancer 1 2 Completed Treatment Healthy Subjects (HS) 1 2 Completed Treatment Hot Flashes 1 2 Completed Treatment Neoplasms of the Prostate 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, film coated Oral Kit; tablet, film coated Oral Tablet Oral - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US7732430 No 2010-06-08 2025-03-02 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 233-236 https://www.chemicalbook.com/ChemicalProductProperty_EN_CB1210710.htm boiling point (°C) 491.9±45.0 https://www.chemicalbook.com/ChemicalProductProperty_EN_CB1210710.htm logP 2.62 https://www.embopress.org/doi/full/10.15252/emmm.201404112 pKa 10.22±0.70 https://www.chemicalbook.com/ChemicalProductProperty_EN_CB1210710.htm - Predicted Properties
Property Value Source logP 1.67 Chemaxon pKa (Strongest Acidic) 10.33 Chemaxon pKa (Strongest Basic) -3.3 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 4 Chemaxon Polar Surface Area 80.92 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 82.55 m3·mol-1 Chemaxon Polarizability 33.88 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- AgonistModulatorRegulator
- General Function
- Zinc ion binding
- Specific Function
- Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissu...
- Gene Name
- ESR1
- Uniprot ID
- P03372
- Uniprot Name
- Estrogen receptor
- Molecular Weight
- 66215.45 Da
References
- Gaspard U, Taziaux M, Mawet M, Jost M, Gordenne V, Coelingh Bennink HJT, Lobo RA, Utian WH, Foidart JM: A multicenter, randomized study to select the minimum effective dose of estetrol (E4) in postmenopausal women (E4Relief): part 1. Vasomotor symptoms and overall safety. Menopause. 2020 Aug;27(8):848-857. doi: 10.1097/GME.0000000000001561. [Article]
- Abot A, Fontaine C, Buscato M, Solinhac R, Flouriot G, Fabre A, Drougard A, Rajan S, Laine M, Milon A, Muller I, Henrion D, Adlanmerini M, Valera MC, Gompel A, Gerard C, Pequeux C, Mestdagt M, Raymond-Letron I, Knauf C, Ferriere F, Valet P, Gourdy P, Katzenellenbogen BS, Katzenellenbogen JA, Lenfant F, Greene GL, Foidart JM, Arnal JF: The uterine and vascular actions of estetrol delineate a distinctive profile of estrogen receptor alpha modulation, uncoupling nuclear and membrane activation. EMBO Mol Med. 2014 Oct;6(10):1328-46. doi: 10.15252/emmm.201404112. [Article]
- Benoit T, Valera MC, Fontaine C, Buscato M, Lenfant F, Raymond-Letron I, Tremollieres F, Soulie M, Foidart JM, Game X, Arnal JF: Estetrol, a Fetal Selective Estrogen Receptor Modulator, Acts on the Vagina of Mice through Nuclear Estrogen Receptor alpha Activation. Am J Pathol. 2017 Nov;187(11):2499-2507. doi: 10.1016/j.ajpath.2017.07.013. Epub 2017 Aug 19. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Zinc ion binding
- Specific Function
- Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent m...
- Gene Name
- ESR2
- Uniprot ID
- Q92731
- Uniprot Name
- Estrogen receptor beta
- Molecular Weight
- 59215.765 Da
References
- Montt-Guevara MM, Giretti MS, Russo E, Giannini A, Mannella P, Genazzani AR, Genazzani AD, Simoncini T: Estetrol Modulates Endothelial Nitric Oxide Synthesis in Human Endothelial Cells. Front Endocrinol (Lausanne). 2015 Jul 22;6:111. doi: 10.3389/fendo.2015.00111. eCollection 2015. [Article]
Enzymes
- 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Glucuronosyltransferase activity
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol su...
- Gene Name
- UGT2B7
- Uniprot ID
- P16662
- Uniprot Name
- UDP-glucuronosyltransferase 2B7
- Molecular Weight
- 60694.12 Da
References
- Gall WE, Zawada G, Mojarrabi B, Tephly TR, Green MD, Coffman BL, Mackenzie PI, Radominska-Pandya A: Differential glucuronidation of bile acids, androgens and estrogens by human UGT1A3 and 2B7. J Steroid Biochem Mol Biol. 1999 Jul-Aug;70(1-3):101-8. doi: 10.1016/s0960-0760(99)00088-6. [Article]
- FDA Approved Drug Products: NEXTSTELLIS (drospirenone and estetrol) tablets for oral use [Link]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- FDA Approved Drug Products: NEXTSTELLIS (drospirenone and estetrol) tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Not Available
- Specific Function
- Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
- Gene Name
- ORM1
- Uniprot ID
- P02763
- Uniprot Name
- Alpha-1-acid glycoprotein 1
- Molecular Weight
- 23511.38 Da
References
- Product monograph: Nexstellis (estetrol and drospirenone) oral tablets [Link]
Drug created at October 20, 2016 21:41 / Updated at April 23, 2021 09:38