Palovarotene
Identification
- Summary
Palovarotene is a selective agonist of retinoic acid receptor gamma (RARγ) used to reduce heterotopic ossification in patients with Fibrodysplasia Ossificans Progressiva (FOP).
- Generic Name
- Palovarotene
- DrugBank Accession Number
- DB05467
- Background
Fibrodysplasia Ossificans Progressiva (FOP), with an estimated worldwide prevalence of one in 2 million individuals, is an exceptionally rare genetic disorder.3 FOP is caused by a gain-of-function mutation in the ACVR1/ALK2 gene which results in progressive heterotopic ossification, a process wherein connective tissues (e.g. skeletal muscle, ligaments, tendons) are replaced with bone.3 The ossification occurring as a result of FOP is insidious and cumulative and is provoked during flare-ups or in response to injury. Treatment options for patients with FOP are extremely limited, although there has been substantial recent interest in novel treatments for this disease.3
Palovarotene is a selective agonist of retinoic acid receptor gamma (RARγ) belonging to a class of medications known as retinoids, similar in mechanism to drugs like tazarotene or trifarotene, which are derivatives of vitamin A. It first garnered interest as a potential treatment for emphysema but was eventually recognized as a potential novel therapy for patients with FOP.1,2,3 Agonists for retinoic acid receptors have been shown to inhibit chondrogenesis of heterotopic ossification in a transgenic mice model of FOP, with selective RARγ agonists (e.g. palovarotene) demonstrating the greatest efficacy.3
Palovarotene was approved for use in Canada in January 2022 for the management of heterotopic ossification (HO) in patients with FOP, representing the first global approval for any FOP therapy.4,6 It has been granted rare pediatric disease and breakthrough therapy designations from the US FDA, although a previously submitted NDA was withdrawn in August 2021 pending the resubmission of additional data analyses.5 On August 16, 2023, palovarotene was also approved by the FDA for the management of HO associated with FOP.9
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 414.549
Monoisotopic: 414.230728214 - Chemical Formula
- C27H30N2O2
- Synonyms
- Palovarotene
- External IDs
- R-667
- R667
- RG-667
- RO3300074
Pharmacology
- Indication
Palovarotene is indicated in Canada to reduce the formation of heterotopic ossification in adults and children (≥8 years old for females and ≥10 years old for males) with Fibrodysplasia Ossificans Progressiva (FOP) by Health Canada and FDA.4,7
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 Management of Heterotopic ossification (ho) •••••••••••• •••••• ••••••••• ••••••• Management of Heterotopic ossification (ho) •••••••••••• •••••• ••••••••• ••••••• Management of Heterotopic ossification (ho) •••••••••••• •••••• ••••••••• ••••••• Management of Heterotopic ossification (ho) •••••••••••• •••••• ••••••••• ••••••• - 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
Palovarotene exerts its pharmacologic effects by inhibiting the pathway(s) responsible for heterotopic ossification in patients with FOP.4 It is orally bioavailable and can be administered once daily, with allowances for short-term increases in dosage in the event of a flare-up.4
As with other retinoids, palovarotene can cause birth defects, and it should not be used by patients who are, or intend to become, pregnant. Palovarotene is contraindicated in patients of childbearing potential unless a number of pregnancy prevention strategies are met (e.g. effective contraception, regular pregnancy testing).4
Palovarotene may also cause a premature physeal closure in growing children. Physeal growth plates should be monitored every 3 months throughout therapy, or more frequently if evidence of adverse effects on growth are observed.4
At doses up to 2.5 times the maximum recommended dose, palovarotene does not prolong the QT interval to any clinically relevant extent.7
Palovarotene binds to retinoic acid receptor gamma (RARγ) with a 10-fold greater affinity compared to retinoic acid receptor alpha or beta. In animal models of Fibrodysplasia Ossificans Progressiva (BMP implant in WT mouse, Q207D mouse model, R206H mouse model), palovarotene decreased heterotopic ossification (HO) in a dose-dependent manner as well as inflammatory and fibroproliferative responses at the sites of injury. Additionally, palovarotene also outperformed corticosteroids in preventing HO, with a dexamethasone treatment of 4.4 mg/kg/day for 4 days demonstrating no clinical efficacy on heterotropic bone volume.8
- Mechanism of action
The pathogenesis of FOP is driven by a gain-of-function mutation in the ACVR1/ALK2 gene encoding activin A receptor type 1 (ACVR1)/activin-like kinase 2 (ALK2), a bone morphogenetic protein type 1 receptor (BMPR-I).3 BMP signalling begins with the complexation of BMPR-II and BMPR-I, which initiates an intracellular signalling pathway mediated by phosphorylated SMAD proteins. The sustained and aberrant signalling caused by the gain-of-function mutation in ACVR1/ALK2 results in overactivation of the downstream SMAD1/5/8 signalling pathway, which in turn is thought to trigger the formation of ectopic chondrogenesis, osteogenesis, and joint fusion characteristic of FOP.3
Palovarotene is a selective agonist of retinoic acid receptor gamma (RARγ), a receptor expressed in chondrogenic cells and chondrocytes that acts as a transcriptional repressor.4 In binding to RARγ, palovarotene decreases BMP signalling and subsequently inhibits the SMAD1/5/8 signalling pathway. Palovarotene's interference with these pathways inhibits chondrogenesis and allows for normal muscle tissue repair to take place, ultimately reducing damage to muscle tissue.4
Target Actions Organism ARetinoic acid receptor gamma agonistHumans - Absorption
Following oral administration of 20mg once daily in healthy adult subjects, the median Tmax was 4.6 hours, the mean Cmax was 140 ng/mL, and the mean AUC(0-τ) was 942 ng*hr/mL.4 At steady-state, the mean trough concentration of palovarotene was 3.5 ng/mL.4
The administration of palovarotene with a high-fat, high-calorie meal resulted in an approximate 40% increase in AUC, an approximate 16% increase in Cmax, and a delay in Tmax by approximately 2 hours when compared to its administration under fasting conditions.4
- Volume of distribution
The mean (SD) apparent volume of distribution (Vd/F) is 237 (± 90.1) L following the administration of a single 20 mg dose with food.7
- Protein binding
The protein binding of palovarotene is 97.9% to 99.6% in vitro.7
- Metabolism
Palovarotene undergoes extensive metabolism by CYP3A4 and, to a lesser extent, CYP2C8 and CYP2C19.4 Five metabolites have been observed in plasma: M1 (6,7-dihydroxy), M2 (6-hydroxy), M3 (7-hydroxy), M4a (6-oxo), and M4b (7-oxo).4 Following oral administration of palovarotene, the parent drug and its four main metabolites (M2, M3, M4a, and M4b) account for approximately 40% of total plasma exposure.4
The metabolites of palovarotene are functionally inactive, with M3 and M4b carrying 1.7% and 4.2% of the activity of their parent compound, respectively.4
- Route of elimination
Following the administration of a 1mg radiolabeled dose of palovarotene in healthy subjects, approximately 97.1% of the administered radioactivity was recovered in the feces, with only 3.2% recovered in the urine.4
- Half-life
The mean elimination half-life of palovarotene at steady-state is 8.7 hours.4
- Clearance
The apparent total body clearance of palovarotene is approximately 19.9 L/h.4
- Adverse Effects
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- Toxicity
Palovarotene is contraindicated during pregnancy. Based on the findings in animal studies and class effects of retinoids, SOHONOS can cause fetal harm when administered during pregnancy. In animal reproduction studies, oral administration of palovarotene to pregnant rats during the period of organogenesis resulted in multiple fetal malformations typical of retinoids (e.g., cleft palate, malformed skull bone, shortening of the long bones) at doses ≥0.25 mg/kg/day (less than the clinical exposure). There are no available human data on palovarotene use in pregnant women. If pregnancy occurs during treatment with palovarotene, discontinue treatment immediately and refer the patient to an obstetrician/gynecologist or other specialist experienced in reproductive toxicity for further evaluation and counseling.7
No clinical experience with an overdose of palovarotene has been reported. Palovarotene is a derivative of vitamin A. In case of accidental overdose, signs of hypervitaminosis A could appear, including severe headache, nausea or vomiting, drowsiness, irritability, and pruritus. Any overdose should be treated with supportive care according to the signs and symptoms exhibited by the patient. If an overdose is suspected, patients should be treated with supportive care as clinically indicated.7
Long-term studies to assess the carcinogenic potential of palovarotene have not been conducted. Palovarotene and its metabolites were negative in the vitro bacterial reverse mutation (Ames) assay and an in vitro micronucleus assay in primary human lymphocyte. Palovarotene did not have any clastogenic effect in the in vivo mouse micronucleus study.7
Palovarotene effects on fertility and reproductive function were assessed in male and female rats. In a female rat fertility study, palovarotene was orally administered to females for 14 days prior to mating with drug naïve males and up to GD 7 at the dose levels of 0.3, 1, and 3 mg/kg/day. Palovarotene caused prolonged periods of diestrous and reduced ovulation rate, resulting in lower numbers of implantation sites and live embryos at 3 mg/kg/day, a dose associated with maternal toxicity.7
In a male rat fertility study, palovarotene was orally administered prior to mating, during mating, and up to scheduled euthanasia (approximately 11 weeks in total) at 0.3, 1, and 3 mg/kg/day. Palovarotene did not cause adverse effects on mating, fertility indices, conception rate, reproductive organ weights, or sperm parameters up to 1 mg/kg/day (less than the clinical exposure). Males did not tolerate 3 mg/kg/day, as it produced severe systemic toxicity including deaths, adverse skin and hair coat clinical signs, and substantially reduced body weight.7
- 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 Palovarotene can be increased when it is combined with Abametapir. Abemaciclib The metabolism of Abemaciclib can be increased when combined with Palovarotene. Acalabrutinib The metabolism of Acalabrutinib can be increased when combined with Palovarotene. Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Palovarotene. Acitretin The risk or severity of adverse effects can be increased when Acitretin is combined with Palovarotene. - Food Interactions
- Avoid grapefruit products. Grapefruit-containing products may inhibit the CYP3A4 activity responsible for palovarotene metabolism.
- Avoid St. John's Wort. The significant induction of CYP3A4 metabolism caused by St. John's wort may decrease the effectiveness of palovarotene.
- Take with food. Co-administration with food increases the oral absorption of palovarotene.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Sohonos Capsule 2.5 mg Oral Ipsen Biopharmaceuticals Canada Inc 2022-06-20 Not applicable Canada Sohonos Capsule 1.5 mg/1 Oral Ipsen Biopharmaceuticals, Inc. 2023-08-16 Not applicable US Sohonos Capsule 10 mg Oral Ipsen Biopharmaceuticals Canada Inc 2022-06-20 Not applicable Canada Sohonos Capsule 5 mg/1 Oral Ipsen Biopharmaceuticals, Inc. 2023-08-16 Not applicable US Sohonos Capsule 10 mg/1 Oral Ipsen Biopharmaceuticals, Inc. 2023-08-16 Not applicable US
Categories
- ATC Codes
- M09AX11 — Palovarotene
- Drug Categories
- BCRP/ABCG2 Inhibitors
- Benzene Derivatives
- Benzylidene Compounds
- BSEP/ABCB11 Inhibitors
- Cytochrome P-450 CYP2B6 Inducers
- Cytochrome P-450 CYP2B6 Inducers (strength unknown)
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2C8 Substrates
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (strength unknown)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Substrates
- Musculo-Skeletal System
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B3 inhibitors
- OCT1 inhibitors
- Retinoids
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as stilbenes. These are organic compounds containing a 1,2-diphenylethylene moiety. Stilbenes (C6-C2-C6 ) are derived from the common phenylpropene (C6-C3) skeleton building block. The introduction of one or more hydroxyl groups to a phenyl ring lead to stilbenoids.
- Kingdom
- Organic compounds
- Super Class
- Phenylpropanoids and polyketides
- Class
- Stilbenes
- Sub Class
- Not Available
- Direct Parent
- Stilbenes
- Alternative Parents
- Tetralins / Benzoic acids / Styrenes / Benzoyl derivatives / Pyrazoles / Heteroaromatic compounds / Carboxylic acids / Azacyclic compounds / Organooxygen compounds / Organonitrogen compounds show 2 more
- Substituents
- Aromatic heteropolycyclic compound / Azacycle / Azole / Benzenoid / Benzoic acid / Benzoic acid or derivatives / Benzoyl / Carboxylic acid / Carboxylic acid derivative / Heteroaromatic compound show 12 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 28K6I5M16G
- CAS number
- 410528-02-8
- InChI Key
- YTFHCXIPDIHOIA-DHZHZOJOSA-N
- InChI
- InChI=1S/C27H30N2O2/c1-26(2)12-13-27(3,4)24-17-22(18-29-15-5-14-28-29)21(16-23(24)26)11-8-19-6-9-20(10-7-19)25(30)31/h5-11,14-17H,12-13,18H2,1-4H3,(H,30,31)/b11-8+
- IUPAC Name
- 4-[(1E)-2-{5,5,8,8-tetramethyl-3-[(1H-pyrazol-1-yl)methyl]-5,6,7,8-tetrahydronaphthalen-2-yl}ethenyl]benzoic acid
- SMILES
- CC1(C)CCC(C)(C)C2=C1C=C(CN1C=CC=N1)C(\C=C\C1=CC=C(C=C1)C(O)=O)=C2
References
- Synthesis Reference
Desjardins, C., Grogan, D. R., Packman, J. N., & Harnett, M. (2017). Methods for treating heterotopic ossification (WO2017210792A1). World Intellectual Property Organization. https://patents.google.com/patent/WO2017210792A1
- General References
- Chiu YY, Roth MD, Kolis S, Rogovitz D, Davies B: Pharmacokinetics of a novel agent, R667, in patients with emphysema. Br J Clin Pharmacol. 2007 May;63(5):527-33. Epub 2007 Feb 23. [Article]
- Brennan B, Chiu Y, Berthelon L, Kolis S, Davies B: Effect of age and gender on the pharmacokinetics of R667, a novel agent for the treatment of emphysema, in healthy volunteers. J Pharm Pharm Sci. 2007;10(1):9-16. [Article]
- Kitoh H: Clinical Aspects and Current Therapeutic Approaches for FOP. Biomedicines. 2020 Sep 2;8(9). pii: biomedicines8090325. doi: 10.3390/biomedicines8090325. [Article]
- Health Canada Product Monograph: Sohonos (palovarotene) capsules for oral use [Link]
- Ipsen: Ipsen announces withdrawal of palovarotene NDA, confirming intention to re-submit following additional data analyses [Link]
- Ipsen Press Release: Health Canada approves Ipsen’s Sohonos (palovarotene capsules) as the first approved treatment for fibrodysplasia ossificans progressiva [Link]
- FDA Approved Drug Products: SOHONOS (palovarotene) capsules, for oral use [Link]
- PALOVAROTENE FOR THE PREVENTION OF HETEROTOPIC OSSIFICATION IN ADULTS AND CHILDREN (≥ 8 YEARS OF AGE FOR FEMALES AND ≥ 10 YEARS OF AGE FOR MALES) WITH FIBRODYSPLASIA OSSIFICANS PROGRESSIVA (FOP) [Link]
- US FDA approves Ipsen’s SohonosTM (palovarotene) capsules, the first and only treatment for people with fibrodysplasia ossificans progressiva [Link]
- External Links
- ChemSpider
- 8470763
- ChEBI
- 188559
- ChEMBL
- CHEMBL2105648
- ZINC
- ZINC000038467831
- Wikipedia
- Palovarotene
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 3 Active Not Recruiting Treatment Fibrodysplasia Ossificans Progressiva (FOP) 1 3 Completed Treatment Fibrodysplasia Ossificans Progressiva (FOP) 1 2 Completed Treatment Fibrodysplasia Ossificans Progressiva (FOP) 3 2 Terminated Treatment Exostoses, Multiple Hereditary 1 2 Terminated Treatment Fibrodysplasia Ossificans Progressiva (FOP) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Capsule Oral 1 mg/1 Capsule Oral 1 mg Capsule Oral 1.5 mg/1 Capsule Oral 1.5 mg Capsule Oral 10 mg/1 Capsule Oral 10 mg Capsule Oral 2.5 mg/1 Capsule Oral 2.5 mg Capsule Oral 5 mg/1 Capsule Oral 5 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US11622959 No 2017-06-08 2037-06-08 US US10864194 No 2020-12-15 2037-06-08 US US10292954 No 2019-05-21 2031-08-31 US US9789074 No 2017-10-17 2031-08-31 US US9314439 No 2016-04-19 2031-08-31 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility 0.04 μg/mL L39990 - Predicted Properties
Property Value Source Water Solubility 0.000344 mg/mL ALOGPS logP 6.94 ALOGPS logP 6.75 Chemaxon logS -6.1 ALOGPS pKa (Strongest Acidic) 4.13 Chemaxon pKa (Strongest Basic) 2.07 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 55.12 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 137.81 m3·mol-1 Chemaxon Polarizability 47.96 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No 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 splash10-0002-0009000000-a6ce01a8a83cafa8e72f Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-03di-0002900000-5ee0f1f1892b39eac36c Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-02t9-0019200000-e2797bb29192f110fd60 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0002-0009000000-f431e12383f698099565 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0pbc-1149000000-22c2a613333184727f8c Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-004j-2119000000-ad42854cf8ca0e5d8232 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]- 200.17332 predictedDeepCCS 1.0 (2019) [M+H]+ 202.5689 predictedDeepCCS 1.0 (2019) [M+Na]+ 208.48141 predictedDeepCCS 1.0 (2019)
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Zinc ion binding
- Specific Function
- Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expressi...
- Gene Name
- RARG
- Uniprot ID
- P13631
- Uniprot Name
- Retinoic acid receptor gamma
- Molecular Weight
- 50341.405 Da
References
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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...
- 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
- 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inducer
- 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: SOHONOS (palovarotene) capsules, for oral use [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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
- PALOVAROTENE FOR THE PREVENTION OF HETEROTOPIC OSSIFICATION IN ADULTS AND CHILDREN (≥ 8 YEARS OF AGE FOR FEMALES AND ≥ 10 YEARS OF AGE FOR MALES) WITH FIBRODYSPLASIA OSSIFICANS PROGRESSIVA (FOP) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- 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
- PALOVAROTENE FOR THE PREVENTION OF HETEROTOPIC OSSIFICATION IN ADULTS AND CHILDREN (≥ 8 YEARS OF AGE FOR FEMALES AND ≥ 10 YEARS OF AGE FOR MALES) WITH FIBRODYSPLASIA OSSIFICANS PROGRESSIVA (FOP) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- 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
- PALOVAROTENE FOR THE PREVENTION OF HETEROTOPIC OSSIFICATION IN ADULTS AND CHILDREN (≥ 8 YEARS OF AGE FOR FEMALES AND ≥ 10 YEARS OF AGE FOR MALES) WITH FIBRODYSPLASIA OSSIFICANS PROGRESSIVA (FOP) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Secondary active organic cation transmembrane transporter activity
- Specific Function
- Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
- Gene Name
- SLC22A1
- Uniprot ID
- O15245
- Uniprot Name
- Solute carrier family 22 member 1
- Molecular Weight
- 61153.345 Da
References
- PALOVAROTENE FOR THE PREVENTION OF HETEROTOPIC OSSIFICATION IN ADULTS AND CHILDREN (≥ 8 YEARS OF AGE FOR FEMALES AND ≥ 10 YEARS OF AGE FOR MALES) WITH FIBRODYSPLASIA OSSIFICANS PROGRESSIVA (FOP) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Transporter activity
- Specific Function
- Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
- Gene Name
- ABCB11
- Uniprot ID
- O95342
- Uniprot Name
- Bile salt export pump
- Molecular Weight
- 146405.83 Da
References
- PALOVAROTENE FOR THE PREVENTION OF HETEROTOPIC OSSIFICATION IN ADULTS AND CHILDREN (≥ 8 YEARS OF AGE FOR FEMALES AND ≥ 10 YEARS OF AGE FOR MALES) WITH FIBRODYSPLASIA OSSIFICANS PROGRESSIVA (FOP) [Link]
Drug created at January 31, 2022 20:47 / Updated at August 23, 2023 22:19