Identification
- Summary
Ulipristal is a selective progesterone receptor modulator used for emergency contraception after unprotected intercourse or in a situation where a planned method of contraception has failed.
- Brand Names
- Ella, Ellaone, Esmya
- Generic Name
- Ulipristal
- DrugBank Accession Number
- DB08867
- Background
Ulipristal is a selective progesterone receptor modulator used for the purposes of emergency contraception (Ella) and for the treatment of uterine fibroids (Fibristal). It is a derivative of 19-norprogesterone and has both antagonistic and partial agonist activity at the progesterone receptor. It also binds to glucocorticoid receptor, however compared to mifepristone (a progesterone receptor antagonist), ulipristal is more tolerable and has lower glucocorticoid activity and better binding affinity.
Ulipristal is currently recommended as first line therapy for emergency contraception, due to improved efficacy and similar side effect profile as compared to the traditional use of levonorgestrel or the Yuzpe regimen. The exact mechanism of action for ulipristal is still currently debated, though there is evidence that it functions by inhibiting ovulation. A recent systematic review proclaimed that the majority of available evidence demonstrates an inhibitory effect on ovulation rather than a post-fertilization effect on the endometrium, which has been heavily debated due to ethical concerns related to abortion (Rosato et al, 2016). Nevertheless, current and ongoing research into the agent's mechanism of action as an emergency contraceptive continue to provide potentially plausible evidence that ulipristal may, in fact, elicit activity on the endometrium that prevents embryo implantation 10,11,12.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Ulipristal (DB08867)
- Weight
- Average: 433.592
Monoisotopic: 433.261693991 - Chemical Formula
- C28H35NO3
- Synonyms
- Ulipristal
- External IDs
- CDB 2914
- CDB-2914
- CDB2914
Pharmacology
- Indication
As the product Ella (available in Canada and the US), ulipristal is indicated for use as emergency contraception after unprotected intercourse or possible contraceptive failure when administered within 120 hours (5 days) after unprotected intercourse or a known or suspected contraceptive failure. As the product Fibristal (available in Canada), ulipristal is indicated for treatment of the signs and symptoms of uterine fibroids in adult women.
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 Symptomatic treatment of Moderate uterine fibroids •••••••••••• ••••• Symptomatic treatment of Moderate uterine fibroids •••••••••••• ••••• Symptomatic treatment of Severe uterine fibroids •••••••••••• ••••• Symptomatic treatment of Severe uterine fibroids •••••••••••• ••••• - Associated Therapies
- Contraindications & Blackbox Warnings
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Ulipristal is a selective, reversible progestin receptor modulator and its tissue targets include the uterus, cervix, ovaries, and hypothalamus. Ulipristal may act as an agonist or antagonist in the presence or absence of progesterone based on the tissue target. If given mid-follicular phase, development of the follicle growth is delayed and estradiol concentrations decrease. If given at the time when luteinizing hormone peaks, follicular rapture is delayed by several days. If given early-luteal phase, a decrease in endometrial thickness can be observed.
- Mechanism of action
The exact mechanism of action of ulipristal has been heavily debated Label 9,10,11,12. On one hand, the majority of official prescribing information labels, monographs, and prior research studies for ulipristal indicated as an emergency contraceptive suggest that its primary mechanism of action revolves around inhibiting or delaying ovulation by suppressing surges in LH that result in the postponement of follicular rupture 9,13,16.
Conversely, some of the latest investigations pertaining to ulipristal's mechanism of action as an emergency contraceptive propose that it principally elicits its action by preventing embryo implantation, as opposed to preventing ovulation 10,11,12. Although previous investigations have shown that ulipristal essentially has the ability to prevent ovulation equivalent to placebo (ie. null effect or ability) when administered during LH peaks one to two days before ovulation, the agent still demonstrates a stable and consistently high contraceptive effect of approximately >=80% when used at this time 10. Subsequently, current studies attempt to investigate how ulipristal could elicit emergency contraception via ovulation prevention under circumstances where ovulation had already clearly been observed 10,11,12. Endometrial biopsy samples studied from such circumstances in such investigations subsequently show that the administered ulipristal causes endometrial tissue to become inhospitable and unsuitable for embryo implantation where a variety of genes characteristic of receptive, pro-gestational endometrium are downregulated 10,11,12.
Nevertheless, most if not all proposed mechanisms commonly agree that ulipristal ultimately demonstrates its pharmacological effects by binding to human progesterone receptors and prevents natural, endogenous progesterone from occupying such receptors 9,13,16,10,11,12. Regardless, however, considering current and on-going research into ulipristal's ability to prevent embryo implantation, the notion that the medication can elicit post-fertilization effects potentially raises alerts and/or ethical debates over the use of ulipristal owing to potential abortifacient activity 9,10,11,12, which is considered to be on par or equipotent to that of mifepristone 15. Attention should be drawn to the fact that some prescribing information, however, such as the US FDA label for ulipristal indicated for emergency contraception, has included new supplementary commentary since 2018 that directly warns about ulipristal not being indicated for termination of existing pregnancies and suggesting that ulipristal use may confer alterations to the endometrium that may affect implantation and contribute to efficacy Label.
In the treatment of fibroids, ulipristal has been shown to exert direct actions on fibroids reducing their size through inhibition of cell proliferation and induction of apoptosis.
Target Actions Organism AProgesterone receptor modulatorHumans AGlucocorticoid receptor antagonistHumans UAndrogen receptor Not Available Humans - Absorption
Tmax, healthy subjects, single oral dose = 60-90 minutes; Cmax, healthy subjects, single oral dose = 176 ± 89 ng/mL; AUC(0-∞), healthy subjects, single oral dose = 556 ± 260 ng·h/mL;
- Volume of distribution
Not Available
- Protein binding
>94% bound to plasma proteins such as albumin, alpha1-acid glycoprotein, lipoproteins (VLDL, LDL, and HDL- due to its lipophillic nature)
- Metabolism
Ulipristal is metabolized by CYP3A4 and to a lesser extent by CYP1A2 into mono-demethylated (active) and di-methylated (inactive) metabolites.
- Route of elimination
Not Available
- Half-life
Mean elimination half-life, single oral dose, healthy subject = 32.4 ± 6.3 hours
- Clearance
Mean oral clearance, single oral dose, healthy subject (CL/F) = 76.8 ± 64.0L/h
- Adverse Effects
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Not Available
- 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 softwareAbametapir The serum concentration of Ulipristal can be increased when it is combined with Abametapir. Abciximab The therapeutic efficacy of Abciximab can be decreased when used in combination with Ulipristal. Acenocoumarol The therapeutic efficacy of Acenocoumarol can be decreased when used in combination with Ulipristal. Acetaminophen The metabolism of Ulipristal can be increased when combined with Acetaminophen. Acetazolamide The metabolism of Ulipristal can be increased when combined with Acetazolamide. - Food Interactions
- Take with or without food. High-fat food increases drug absorption, but not to a clinically significant extent.
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 Ulipristal acetate YF7V70N02B 126784-99-4 OOLLAFOLCSJHRE-ZHAKMVSLSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ella Tablet 30 mg/1 Oral HRA Pharma America, Inc. 2020-05-11 Not applicable US 
Ella Tablet 30 mg/1 Oral Afaxys Pharma Llc 2010-08-13 Not applicable US Ella Tablet 30 mg/1 Oral CENEXI HSC 2020-05-11 Not applicable US Ella Tablet 30 mg/1 Oral A-S Medication Solutions 2020-05-11 Not applicable US Ella Tablet 30 mg/1 Oral Rpk Pharmaceuticals, Inc. 2010-08-13 Not applicable US
Categories
- ATC Codes
- G03AD02 — Ulipristal
- G03AD — Emergency contraceptives
- G03A — HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE
- G03 — SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
- G — GENITO URINARY SYSTEM AND SEX HORMONES
- Drug Categories
- Adrenal Cortex Hormones
- Contraceptive Agents, Female
- Contraceptive Agents, Hormonal
- Contraceptives, Postcoital
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Fused-Ring Compounds
- Genito Urinary System and Sex Hormones
- Hormonal Contraceptives for Systemic Use
- Norpregnanes
- Norsteroids
- Progesterone Agonist/Antagonist
- Progesterone Receptor Modulators
- Reproductive Control Agents
- Selective Progesterone Receptor Modulators
- Sex Hormones and Modulators of the Genital System
- Steroids
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as 20-oxosteroids. These are steroid derivatives carrying a C=O group at the 20-position of the steroid skeleton.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Steroids and steroid derivatives
- Sub Class
- Oxosteroids
- Direct Parent
- 20-oxosteroids
- Alternative Parents
- 3-oxosteroids / 17-hydroxysteroids / Dialkylarylamines / Aniline and substituted anilines / Cyclohexenones / Tertiary alcohols / Alpha-hydroxy ketones / Cyclic alcohols and derivatives / Organopnictogen compounds / Organic oxides show 1 more
- Substituents
- 17-hydroxysteroid / 20-oxosteroid / 3-oxosteroid / Alcohol / Alpha-hydroxy ketone / Amine / Aniline or substituted anilines / Aromatic homopolycyclic compound / Benzenoid / Carbonyl group show 17 more
- Molecular Framework
- Aromatic homopolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 6J5J15Q2X8
- CAS number
- 159811-51-5
- InChI Key
- HKDLNTKNLJPAIY-WKWWZUSTSA-N
- InChI
- InChI=1S/C28H35NO3/c1-17(30)28(32)14-13-25-23-11-7-19-15-21(31)10-12-22(19)26(23)24(16-27(25,28)2)18-5-8-20(9-6-18)29(3)4/h5-6,8-9,15,23-25,32H,7,10-14,16H2,1-4H3/t23-,24+,25-,27-,28-/m0/s1
- IUPAC Name
- (10S,11S,14R,15S,17R)-14-acetyl-17-[4-(dimethylamino)phenyl]-14-hydroxy-15-methyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-1,6-dien-5-one
- SMILES
- CN(C)C1=CC=C(C=C1)[C@H]1C[C@@]2(C)[C@@H](CC[C@]2(O)C(C)=O)[C@@H]2CCC3=CC(=O)CCC3=C12
References
- General References
- Pohl O, Osterloh I, Gotteland JP: Ulipristal acetate - safety and pharmacokinetics following multiple doses of 10-50 mg per day. J Clin Pharm Ther. 2013 Aug;38(4):314-20. doi: 10.1111/jcpt.12065. Epub 2013 Apr 3. [Article]
- Melis GB, Piras B, Marotto MF, Orru' MM, Maricosu G, Pilloni M, Guerriero S, Angiolucci M, Lello S, Paoletti AM: Pharmacokinetic evaluation of ulipristal acetate for uterine leiomyoma treatment. Expert Opin Drug Metab Toxicol. 2012 Jul;8(7):901-8. doi: 10.1517/17425255.2012.695775. Epub 2012 Jun 10. [Article]
- Gemzell-Danielsson K, Rabe T, Cheng L: Emergency contraception. Gynecol Endocrinol. 2013 Mar;29 Suppl 1:1-14. doi: 10.3109/09513590.2013.774591. [Article]
- Martinez AM, Thomas MA: Ulipristal acetate as an emergency contraceptive agent. Expert Opin Pharmacother. 2012 Sep;13(13):1937-42. doi: 10.1517/14656566.2012.705832. Epub 2012 Jul 7. [Article]
- Maruo T, Ohara N, Matsuo H, Xu Q, Chen W, Sitruk-Ware R, Johansson ED: Effects of levonorgestrel-releasing IUS and progesterone receptor modulator PRM CDB-2914 on uterine leiomyomas. Contraception. 2007 Jun;75(6 Suppl):S99-103. Epub 2007 Mar 21. [Article]
- Creinin MD, Schlaff W, Archer DF, Wan L, Frezieres R, Thomas M, Rosenberg M, Higgins J: Progesterone receptor modulator for emergency contraception: a randomized controlled trial. Obstet Gynecol. 2006 Nov;108(5):1089-97. [Article]
- Blithe DL, Nieman LK, Blye RP, Stratton P, Passaro M: Development of the selective progesterone receptor modulator CDB-2914 for clinical indications. Steroids. 2003 Nov;68(10-13):1013-7. [Article]
- Attardi BJ, Burgenson J, Hild SA, Reel JR: In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone. J Steroid Biochem Mol Biol. 2004 Mar;88(3):277-88. [Article]
- Rosato E, Farris M, Bastianelli C: Mechanism of Action of Ulipristal Acetate for Emergency Contraception: A Systematic Review. Front Pharmacol. 2016 Jan 12;6:315. doi: 10.3389/fphar.2015.00315. eCollection 2015. [Article]
- Mozzanega B, Nardelli GB: UPA and LNG in emergency contraception: the information by EMA and the scientific evidences indicate a prevalent anti-implantation effect. Eur J Contracept Reprod Health Care. 2019 Jan 18:1-7. doi: 10.1080/13625187.2018.1555662. [Article]
- Lira-Albarran S, Durand M, Barrera D, Vega C, Becerra RG, Diaz L, Garcia-Quiroz J, Rangel C, Larrea F: A single preovulatory administration of ulipristal acetate affects the decidualization process of the human endometrium during the receptive period of the menstrual cycle. Mol Cell Endocrinol. 2018 Nov 15;476:70-78. doi: 10.1016/j.mce.2018.04.010. Epub 2018 Apr 27. [Article]
- Lira-Albarran S, Durand M, Larrea-Schiavon MF, Gonzalez L, Barrera D, Vega C, Gamboa-Dominguez A, Rangel C, Larrea F: Ulipristal acetate administration at mid-cycle changes gene expression profiling of endometrial biopsies taken during the receptive period of the human menstrual cycle. Mol Cell Endocrinol. 2017 May 15;447:1-11. doi: 10.1016/j.mce.2017.02.024. Epub 2017 Feb 20. [Article]
- Electronic Medicines Compendium: ellaOne (ulipristal acetate) 30 mg Monograph [Link]
- FDA Approved Drug Products: ELLA (ulipristal acetate) tablets [Link]
- European Medicines Agency CHMP Assessment Report for Ellaone (ulipristal acetate) [File]
- ella (ulipristal acetate) 30 mg Tablet Emergency Contraceptive Canadian Product Monograph [File]
- External Links
- KEGG Drug
- D09567
- PubChem Compound
- 13559281
- PubChem Substance
- 310264902
- ChemSpider
- 19349271
- 1005921
- ChEBI
- 71025
- ChEMBL
- CHEMBL2103846
- ZINC
- ZINC000034089131
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Ulipristal_acetate
- FDA label
- Download (227 KB)
- MSDS
- Download (479 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 Completed Basic Science Contraception 2 4 Completed Treatment Emergency Contraception 1 4 Completed Treatment Induction of Second Trimester Abortion 1 4 Completed Treatment Uterine Fibroids (Leiomyomas) 1 4 Recruiting Treatment Contraceptive Usage 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, film coated Oral Tablet Oral 30 mg/1 Tablet Oral 30 mg Tablet Oral 30.00 mg Tablet, film coated Oral 30 MG Tablet Oral 5.00 mg Tablet Oral 500000 mg Tablet Oral Tablet Oral 5 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8426392 No 2013-04-23 2030-06-12 US US8962603 No 2015-02-24 2030-06-12 US US9283233 No 2016-03-15 2030-04-13 US US8735380 No 2014-05-27 2029-02-20 US US8512745 No 2013-08-20 2030-06-02 US US10159681 No 2018-12-25 2030-04-13 US US9844510 No 2017-12-19 2028-12-08 US US10772897 No 2020-09-15 2030-04-13 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.00943 mg/mL ALOGPS logP 4.45 ALOGPS logP 4.18 Chemaxon logS -4.7 ALOGPS pKa (Strongest Acidic) 12.7 Chemaxon pKa (Strongest Basic) 4.89 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 57.61 Å2 Chemaxon Rotatable Bond Count 3 Chemaxon Refractivity 129.29 m3·mol-1 Chemaxon Polarizability 49.66 Å3 Chemaxon Number of Rings 5 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
Property Value Probability Human Intestinal Absorption + 0.9964 Blood Brain Barrier + 0.6396 Caco-2 permeable + 0.577 P-glycoprotein substrate Substrate 0.6286 P-glycoprotein inhibitor I Inhibitor 0.9708 P-glycoprotein inhibitor II Inhibitor 0.9321 Renal organic cation transporter Non-inhibitor 0.799 CYP450 2C9 substrate Non-substrate 0.8337 CYP450 2D6 substrate Non-substrate 0.8848 CYP450 3A4 substrate Substrate 0.8312 CYP450 1A2 substrate Non-inhibitor 0.5677 CYP450 2C9 inhibitor Non-inhibitor 0.7078 CYP450 2D6 inhibitor Non-inhibitor 0.7827 CYP450 2C19 inhibitor Non-inhibitor 0.6021 CYP450 3A4 inhibitor Inhibitor 0.7866 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6633 Ames test Non AMES toxic 0.8603 Carcinogenicity Non-carcinogens 0.7916 Biodegradation Not ready biodegradable 0.9933 Rat acute toxicity 2.6728 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9538 hERG inhibition (predictor II) Non-inhibitor 0.686
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-014i-0002900000-c273f4efdd9a92186688 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-001i-0001900000-00dd58493c11d10c245a Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-00kb-0439500000-385f183df11bd4efa8fe Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-001l-0006900000-418ce52f8aab98c07854 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-00e9-2078900000-5093bf377acff06b2169 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-001j-1941100000-b67085eded1d6b6c17a5 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 203.87987 predictedDeepCCS 1.0 (2019) [M+H]+ 205.77525 predictedDeepCCS 1.0 (2019) [M+Na]+ 211.40462 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Modulator
- General Function
- Zinc ion binding
- Specific Function
- The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Progesterone receptor ...
- Gene Name
- PGR
- Uniprot ID
- P06401
- Uniprot Name
- Progesterone receptor
- Molecular Weight
- 98979.96 Da
References
- Gemzell-Danielsson K, Rabe T, Cheng L: Emergency contraception. Gynecol Endocrinol. 2013 Mar;29 Suppl 1:1-14. doi: 10.3109/09513590.2013.774591. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Zinc ion binding
- Specific Function
- Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modula...
- Gene Name
- NR3C1
- Uniprot ID
- P04150
- Uniprot Name
- Glucocorticoid receptor
- Molecular Weight
- 85658.57 Da
References
- Gemzell-Danielsson K, Rabe T, Cheng L: Emergency contraception. Gynecol Endocrinol. 2013 Mar;29 Suppl 1:1-14. doi: 10.3109/09513590.2013.774591. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Zinc ion binding
- Specific Function
- Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription ...
- Gene Name
- AR
- Uniprot ID
- P10275
- Uniprot Name
- Androgen receptor
- Molecular Weight
- 98987.9 Da
References
- Gemzell-Danielsson K, Rabe T, Cheng L: Emergency contraception. Gynecol Endocrinol. 2013 Mar;29 Suppl 1:1-14. doi: 10.3109/09513590.2013.774591. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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
- No
- Actions
- Substrate
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- 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 oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Martinez AM, Thomas MA: Ulipristal acetate as an emergency contraceptive agent. Expert Opin Pharmacother. 2012 Sep;13(13):1937-42. doi: 10.1517/14656566.2012.705832. Epub 2012 Jul 7. [Article]
- Pohl O, Zobrist RH, Gotteland JP: The clinical pharmacology and pharmacokinetics of ulipristal acetate for the treatment of uterine fibroids. Reprod Sci. 2015 Apr;22(4):476-83. doi: 10.1177/1933719114549850. Epub 2014 Sep 16. [Article]
- Pohl O, Osterloh I, Gotteland JP: Effects of erythromycin at steady-state concentrations on the pharmacokinetics of ulipristal acetate. J Clin Pharm Ther. 2013 Dec;38(6):512-7. doi: 10.1111/jcpt.12098. Epub 2013 Sep 16. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- 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
Drug created at April 27, 2013 05:33 / Updated at February 20, 2024 23:55