Identification
- Summary
Relugolix is an oral GnRH receptor antagonist for androgen deprivation therapy in the treatment of advanced prostate cancer.
- Brand Names
- Myfembree, Orgovyx
- Generic Name
- Relugolix
- DrugBank Accession Number
- DB11853
- Background
Relugolix is a gonadotropin-releasing hormone (GnRH) receptor antagonist used in the treatment of several hormone-responsive conditions. It was first approved in Japan in 2019, under the brand name Relumina, for the symptomatic treatment of uterine fibroids,6 and more recently by the United States' FDA in 2020, under the brand name Orgovyx, for the treatment of advanced prostate cancer.9,10 This branded product was later approved by the European Commission on April 29, 2022.14 Relugolix has also been studied in the symptomatic treatment of endometriosis.1
Relugolix is the first (and currently only) orally-administered GnRH receptor antagonist approved for the treatment of prostate cancer - similar therapies such as degarelix require subcutaneous administration - and therefore provides a less burdensome therapeutic option for patients who might otherwise require clinic visits for administration by healthcare professionals.10 In addition to its relative ease-of-use, relugolix was shown to be superior in the depression of testosterone levels when compared to leuprolide, another androgen deprivation therapy used in the treatment of prostate cancer.8 In May 2021, the FDA approved the combination product made up of relugolix, estradiol, and norethindrone under the market name Myfembree for the first once-daily treatment for the management of heavy menstrual bleeding associated with uterine fibroids in premenopausal women.12
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Relugolix (DB11853)
- Weight
- Average: 623.64
Monoisotopic: 623.176244497 - Chemical Formula
- C29H27F2N7O5S
- Synonyms
- Relugolix
- External IDs
- TAK 385
- TAK-385
Pharmacology
- Indication
Relugolix is indicated for the treatment of adult patients with advanced prostate cancer.9,13 In a combination product with estradiol and norethindrone, relugolix is indicated for the once-daily treatment for the management of heavy menstrual bleeding associated with uterine fibroids in premenopausal women.12
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 hormone sensitive prostate cancer •••••••••••• ••••• •••••• Treatment of Advanced prostate cancer •••••••••••• ••••• •••••• Used in combination to manage Heavy menstrual bleeding Combination Product in combination with: Norethisterone (DB00717), Estradiol (DB00783) •••••••••••• ••••••••••••• •••••• Used in combination to manage Severe pain Combination Product in combination with: Norethisterone (DB00717), Estradiol (DB00783) •••••••••••• ••••••••••••• •••••• - 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
Approximately 56% of patients achieved castrate-level testosterone concentrations (<50 ng/dL) by day 4 of therapy and 97% of patients maintain these levels through 48 weeks of therapy.9 Relugolix requires once-daily oral administration to maintain the desired testosterone concentrations.
Androgen deprivation therapies may prolong the QTc interval and should therefore be used with caution in patients having a high baseline risk of QTc prolongation, such as those with electrolyte abnormalities, congestive heart failure, or using other medications known to prolong the QTc interval.9 Based on its mechanism of action and data from animal studies, relugolix may result in fetal harm if administered to pregnant females - male patients with female partners should be advised to use effective contraception throughout therapy and for 2 weeks following cessation of therapy to prevent inadvertent fetal exposure.9
- Mechanism of action
The pathogenesis and progression of prostate cancer appear driven, at least in part, by the effects of testosterone.5 Androgen deprivation has been demonstrated to result in cell death and tumor regression in many well-differentiated prostate cancer cell lines - for this reason, androgen deprivation therapy (ADT) has become a standard in the treatment of prostate cancer, particularly in advanced disease.
Testosterone production in males is carried out in the Leydig cells of testes and is stimulated by luteinizing hormone (LH), which itself is produced in the pituitary gland following the binding of gonadotropin-releasing hormone (GnRH) to corresponding GnRH receptors.11 Relugolix is a competitive antagonist of these GnRH receptors, thereby decreasing the release of LH and, ultimately, testosterone.9
Target Actions Organism AGonadotropin-releasing hormone receptor antagonistHumans - Absorption
The Cmax and AUC of orally-administered relugolix increase proportionally following single doses - in contrast, with repeat dosing the AUC remains proportional to the dose while the Cmax increases greater than proportionally to the dose.9 Following the administration of 120mg once daily, the steady-state AUC and Cmax of relugolix were 407 (± 168) ng.hr/mL and 70 (± 65) ng/mL, respectively.
The absolute oral bioavailability of relugolix is approximately 12% and the median Tmax following oral administration is 2.25 hours.9
- Volume of distribution
Not Available
- Protein binding
Relugolix is 68-71% protein-bound in plasma, primarily to albumin and, to a lesser extent, α1-acid glycoprotein.9
- Metabolism
Relugolix is metabolized mainly by the CYP3A subfamily of P450 enzymes, with a smaller contribution by CYP2C8.9
- Route of elimination
Approximately 81% of an orally administered dose was recovered in the feces, of which 4.2% was unchanged parent drug, while 4.1% of the dose was recovered in the urine, of which 2.2% remained unchanged.9
- Half-life
The average effective half-life of relugolix is 25 hours, while the average terminal elimination half-life is 60.8 hours.9
- Clearance
The average renal clearance of relugolix is 8 L/h with a total clearance of 26.4 L/h.9
- 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
Data regarding overdose of relugolix are unavailable.
- 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 Relugolix can be increased when it is combined with Abametapir. Abatacept The metabolism of Relugolix can be increased when combined with Abatacept. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Relugolix. Abrocitinib The serum concentration of Relugolix can be increased when it is combined with Abrocitinib. Acalabrutinib The metabolism of Relugolix can be decreased when combined with Acalabrutinib. - Food Interactions
- Take with or without food. Administration with food does not result in any clinically meaningful differences in pharmacokinetics.
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.- International/Other Brands
- Orgovyx / Relumina
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Orgovyx Tablet, film coated 120 mg Oral Accord Healthcare S.L.U. 2022-05-11 Not applicable EU 
Orgovyx Tablet 120 mg Oral Sumitomo Pharma Switzerland Gmbh Not applicable Not applicable Canada 
Orgovyx Tablet, film coated 120 mg Oral Accord Healthcare S.L.U. 2023-04-04 Not applicable EU Orgovyx Tablet, film coated 120 mg/1 Oral Sumitomo Pharma America, Inc 2020-12-18 Not applicable US 
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Myfembree Relugolix (40 mg) + Estradiol (1 mg) + Norethisterone acetate (0.5 mg) Tablet Oral Sumitomo Pharma Switzerland Gmbh Not applicable Not applicable Canada Myfembree Relugolix (40 mg/1) + Estradiol hemihydrate (1 mg/1) + Norethisterone acetate (0.5 mg/1) Tablet, film coated Oral Sumitomo Pharma America, Inc 2021-05-26 Not applicable US Ryeqo Relugolix (40 mg) + Estradiol hemihydrate (1 mg) + Norethisterone acetate (0.5 mg) Tablet, film coated Oral Gedeon Richter Plc. 2021-10-06 Not applicable EU Ryeqo Relugolix (40 mg) + Estradiol hemihydrate (1 mg) + Norethisterone acetate (0.5 mg) Tablet, film coated Oral Gedeon Richter Plc. 2021-10-06 Not applicable EU
Categories
- ATC Codes
- H01CC54 — Relugolix, estradiol and norethisterone
- H01CC — Anti-gonadotropin-releasing hormones
- H01C — HYPOTHALAMIC HORMONES
- H01 — PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES
- H — SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
- Drug Categories
- Amides
- Anti-Gonadotropin-Releasing Hormones
- Antiandrogens
- Antineoplastic and Immunomodulating Agents
- BCRP/ABCG2 Inhibitors
- Benzene Derivatives
- Cytochrome P-450 CYP2B6 Inducers
- Cytochrome P-450 CYP2B6 Inducers (strength unknown)
- Cytochrome P-450 CYP2C8 Substrates
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 CYP3A7 Substrates
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Substrates
- Decreased GnRH Secretion
- Endocrine Therapy
- Gonadotropin Releasing Hormone Receptor Antagonists
- Gonadotropin-releasing Hormone Antagonists
- Hormone Antagonists
- Hormone Antagonists and Related Agents
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Hypothalamic Hormones
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Pituitary and Hypothalamic Hormones and Analogues
- Potential QTc-Prolonging Agents
- Prostatic Neoplasms, drug therapy
- Pyrimidines
- QTc Prolonging Agents
- Receptors, LHRH, antagonists & inhibitors
- Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as n-phenylureas. These are compounds containing a N-phenylurea moiety, which is structurally characterized by a phenyl group linked to one nitrogen atom of a urea group.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- N-phenylureas
- Direct Parent
- N-phenylureas
- Alternative Parents
- Thienopyrimidines / Pyrimidones / Alkyl aryl ethers / Aralkylamines / Fluorobenzenes / Pyridazines and derivatives / Aryl fluorides / Vinylogous amides / Thiophenes / Heteroaromatic compounds show 8 more
- Substituents
- Alkyl aryl ether / Amine / Aralkylamine / Aromatic heteropolycyclic compound / Aryl fluoride / Aryl halide / Azacycle / Carbonyl group / Ether / Fluorobenzene show 22 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- P76B05O5V6
- CAS number
- 737789-87-6
- InChI Key
- AOMXMOCNKJTRQP-UHFFFAOYSA-N
- InChI
- InChI=1S/C29H27F2N7O5S/c1-36(2)14-19-24-26(39)38(22-12-13-23(42-3)34-33-22)29(41)37(15-18-20(30)6-5-7-21(18)31)27(24)44-25(19)16-8-10-17(11-9-16)32-28(40)35-43-4/h5-13H,14-15H2,1-4H3,(H2,32,35,40)
- IUPAC Name
- 1-(4-{1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1H,2H,3H,4H-thieno[2,3-d]pyrimidin-6-yl}phenyl)-3-methoxyurea
- SMILES
- CONC(=O)NC1=CC=C(C=C1)C1=C(CN(C)C)C2=C(S1)N(CC1=C(F)C=CC=C1F)C(=O)N(C2=O)C1=CC=C(OC)N=N1
References
- Synthesis Reference
Miwa K, Hitaka T, Imada T, Sasaki S, Yoshimatsu M, Kusaka M, Tanaka A, Nakata D, Furuya S, Endo S, Hamamura K, Kitazaki T: Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl )-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor. J Med Chem. 2011 Jul 28;54(14):4998-5012. doi: 10.1021/jm200216q. Epub 2011 Jun 23.
- General References
- Osuga Y, Seki Y, Tanimoto M, Kusumoto T, Kudou K, Terakawa N: Relugolix, an oral gonadotropin-releasing hormone receptor antagonist, reduces endometriosis-associated pain in a dose-response manner: a randomized, double-blind, placebo-controlled study. Fertil Steril. 2020 Sep 7. pii: S0015-0282(20)30716-0. doi: 10.1016/j.fertnstert.2020.07.055. [Article]
- Miwa K, Hitaka T, Imada T, Sasaki S, Yoshimatsu M, Kusaka M, Tanaka A, Nakata D, Furuya S, Endo S, Hamamura K, Kitazaki T: Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl )-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor. J Med Chem. 2011 Jul 28;54(14):4998-5012. doi: 10.1021/jm200216q. Epub 2011 Jun 23. [Article]
- Barra F, Seca M, Della Corte L, Giampaolino P, Ferrero S: Relugolix for the treatment of uterine fibroids. Drugs Today (Barc). 2019 Aug;55(8):503-512. doi: 10.1358/dot.2019.55.8.3020179. [Article]
- MacLean DB, Shi H, Faessel HM, Saad F: Medical Castration Using the Investigational Oral GnRH Antagonist TAK-385 (Relugolix): Phase 1 Study in Healthy Males. J Clin Endocrinol Metab. 2015 Dec;100(12):4579-87. doi: 10.1210/jc.2015-2770. Epub 2015 Oct 26. [Article]
- Michaud JE, Billups KL, Partin AW: Testosterone and prostate cancer: an evidence-based review of pathogenesis and oncologic risk. Ther Adv Urol. 2015 Dec;7(6):378-87. doi: 10.1177/1756287215597633. [Article]
- Markham A: Relugolix: First Global Approval. Drugs. 2019 Apr;79(6):675-679. doi: 10.1007/s40265-019-01105-0. [Article]
- Kittai AS, Blank J, Graff JN: Gonadotropin-Releasing Hormone Antagonists in Prostate Cancer. Oncology (Williston Park). 2018 Dec 17;32(12):599-602, 604-6. [Article]
- Shore ND, Saad F, Cookson MS, George DJ, Saltzstein DR, Tutrone R, Akaza H, Bossi A, van Veenhuyzen DF, Selby B, Fan X, Kang V, Walling J, Tombal B: Oral Relugolix for Androgen-Deprivation Therapy in Advanced Prostate Cancer. N Engl J Med. 2020 Jun 4;382(23):2187-2196. doi: 10.1056/NEJMoa2004325. Epub 2020 May 29. [Article]
- FDA Approved Drug Products: Orgovyx (relugolix) tablets for oral use [Link]
- FDA News Release: FDA Approves First Oral Hormone Therapy for Treating Advanced Prostate Cancer [Link]
- GeekyMedics: How the Gonadal Axis Works [Link]
- FDA Approved Drug Products: MYFEMBREE (relugolix, estradiol, and norethindrone acetate) tablets, for oral use [Link]
- EMA Approved Drug Products: Orgovyx (relugolix) Oral Tablets [Link]
- GlobeNewswire News Release: Myovant Sciences Announces European Commission Approval for ORGOVYX® (relugolix) for the Treatment of Advanced Hormone-Sensitive Prostate Cancer [Link]
- External Links
- PubChem Compound
- 10348973
- PubChem Substance
- 347828195
- ChemSpider
- 8524431
- BindingDB
- 50347982
- 2472778
- ChEMBL
- CHEMBL1800159
- ZINC
- ZINC000043206033
- Wikipedia
- Relugolix
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 Recruiting Treatment Biochemically Recurrent Prostate Carcinoma / Localized Prostate Carcinoma / Stage I Prostate Cancer AJCC v8 / Stage II Prostate Cancer AJCC v8 / Stage IIA Prostate Cancer AJCC v8 / Stage IIB Prostate Cancer AJCC v8 / Stage IIC Prostate Cancer AJCC v8 / Stage III Prostate Cancer AJCC v8 / Stage IIIA Prostate Cancer AJCC v8 / Stage IIIB Prostate Cancer AJCC v8 / Stage IIIC Prostate Cancer AJCC v8 1 4 Recruiting Treatment Hypermenorrhea / Metrorrhagia / Pelvic Pain / Uterine Fibroids (Leiomyomas) 1 3 Active Not Recruiting Treatment Contraception 1 3 Active Not Recruiting Treatment Prostate Cancer 1 3 Completed Treatment Endometriosis 2
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral Tablet, film coated Oral Tablet Oral 120 mg Tablet, film coated Oral 120 mg/1 Tablet, film coated Oral 120 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8735401 No 2014-05-27 2024-02-04 US US10449191 No 2019-10-22 2037-09-29 US US10786501 No 2020-09-29 2037-09-29 US US10350170 No 2019-07-16 2036-02-25 US US8058280 No 2011-11-15 2024-01-28 US US7300935 No 2007-11-27 2024-01-28 US US9346822 No 2016-05-24 2024-02-17 US US11033551 No 2021-06-15 2037-09-29 US US11583526 No 2017-09-29 2037-09-29 US US11793812 No 2018-05-03 2038-05-03 US US11795178 No 2013-09-27 2033-09-27 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.00198 mg/mL ALOGPS logP 3.16 ALOGPS logP 3.94 Chemaxon logS -5.5 ALOGPS pKa (Strongest Acidic) 9.07 Chemaxon pKa (Strongest Basic) 7.69 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 8 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 129.23 Å2 Chemaxon Rotatable Bond Count 9 Chemaxon Refractivity 160.92 m3·mol-1 Chemaxon Polarizability 62.44 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 230.76003 predictedDeepCCS 1.0 (2019) [M+H]+ 232.65543 predictedDeepCCS 1.0 (2019) [M+Na]+ 238.3277 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Peptide binding
- Specific Function
- Receptor for gonadotropin releasing hormone (GnRH) that mediates the action of GnRH to stimulate the secretion of the gonadotropic hormones luteinizing hormone (LH) and follicle-stimulating hormone...
- Gene Name
- GNRHR
- Uniprot ID
- P30968
- Uniprot Name
- Gonadotropin-releasing hormone receptor
- Molecular Weight
- 37730.355 Da
References
- FDA Approved Drug Products: Orgovyx (relugolix) tablets for oral use [Link]
Enzymes
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInducer
- 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...
Components:
| Name | UniProt ID |
|---|---|
| Cytochrome P450 3A4 | P08684 |
| Cytochrome P450 3A43 | Q9HB55 |
| Cytochrome P450 3A5 | P20815 |
| Cytochrome P450 3A7 | P24462 |
References
- FDA Approved Drug Products: Orgovyx (relugolix) tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid 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 oxidizes a variety of structurally un...
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- FDA Approved Drug Products: Orgovyx (relugolix) tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Steroid 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 oxidizes a variety of structurally un...
- Gene Name
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- FDA Approved Drug Products: Orgovyx (relugolix) 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: Orgovyx (relugolix) 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
- FDA Approved Drug Products: Orgovyx (relugolix) tablets for oral use [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- FDA Approved Drug Products: Orgovyx (relugolix) tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- 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: Orgovyx (relugolix) tablets for oral use [Link]
Drug created at October 20, 2016 20:54 / Updated at June 21, 2022 07:09