Sofpironium
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Identification
- Summary
Sofpironium is a topical anticholinergic used to treat primary axillary hyperhidrosis.
- Brand Names
- Sofdra
- Generic Name
- Sofpironium
- DrugBank Accession Number
- DB19325
- Background
Sofpironium is a "soft" anticholinergic analog of glycopyrronium that has been modified with a readily hydrolyzable ester moiety.6 Soft drugs are designed to reduce systemic toxicity while enhancing local efficacy by employing retrometabolic drug design, in which a molecule contains a metabolically sensitive moiety that promotes rapid metabolism to inactive metabolites after exerting activity at its target site.2 Sofpironium is rapidly converted to a less active metabolite, BBI-4010, after exerting its activity, thereby limiting the incidence and/or severity of systemic anticholinergic effects.5,6
Sofpironium bromide (Sofdra) was approved by the FDA in June 2024 for the topical treatment of primary axillary hyperhidrosis.4,5 It has also been available in Japan since 2020 under the brand name Ecclock.4
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 390.499
Monoisotopic: 390.227499555 - Chemical Formula
- C22H32NO5
- Synonyms
- Pyrrolidinium, 3-(((2r)-2-cyclopentyl-2-hydroxy-2-phenylacetyl)oxy)-1-(2-ethoxy-2-oxoethyl)-1-methyl-, (3r)-
- Sofpironium cation
- Sofpironium ion
- External IDs
- BBI-4000 cation
- BBI-4000 ion
Pharmacology
- Indication
Sofpironium bromide is indicated for the treatment of primary axillary hyperhidrosis in patients ≥9 years of age.5
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 Primary axillary hyperhidrosis •••••••••••• •••••• ••••••••• ••• - Contraindications & Blackbox Warnings
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- Pharmacodynamics
Binding studies at human muscarinic receptors (M1–M4) and guinea-pig ileum assays have found sofpironium bromide to have potency close to glycopyrronium with a shorter duration of action.6
Despite its topical application, sofpironium bromide exhibits some degree of systemic absorption that can result in anticholinergic adverse effects like urinary retention and heat illness.5 Patients with conditions that may be exacerbated by anticholinergic agents (e.g. myasthenia gravis, Sjögren’s syndrome) should not use sofpironium bromide, nor should it be used in patients already undergoing treatment with a systemic anticholinergic medication.5
- Mechanism of action
Sofpironium is a competitive inhibitor of muscarinic acetylcholine receptors are located on certain peripheral tissues, including eccrine sweat glands.5 By inhibiting the activity of these receptors, sofpironium indirectly reduces the rate of sweating in patients with axillary hyperhidrosis.
Target Actions Organism AMuscarinic acetylcholine receptor M3 inhibitorHumans AMuscarinic acetylcholine receptor inhibitorHumans - Absorption
Following a single topical administration of sofpironium in adult patients, the mean plasma Cmax was 2.71 ng/mL, the AUC0-t was 45.1 ng.hr/mL, and the tmax was 5.34 hours.5 Following a single topical administration of sofpironium in pediatric patients (9 to 16 years of age), the mean plasma Cmax was 1.30 ng/mL, the AUC0-t was 14.6 ng.hr/mL, and the tmax was 4.0 hours.5
- Volume of distribution
Not Available
- Protein binding
Plasma protein binding of sofpironium is approximately 34.8 - 37.8%.5 Plasma protein binding of BBI-4010 is significantly lower at approximately 2.3 - 3.7%.5
- Metabolism
Sofpironium is metabolized by non-enzymatic hydrolysis, oxidative metabolism via CYP2D6 and CYP3A4, and glycine conjugation.5 As a product of retrometabolic drug design, sofpironium includes a metabolically labile ester moiety that is readily hydrolyzed (by plasma paraoxonase 1 (PON1))3 to produce BBI-4010, a less active anticholinergic agent, thereby limiting the risk of systemic adverse effects.6
In plasma, the major component was sofpironium (38%) followed by BBI-4010 (20%).5
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- Route of elimination
Urinary excretion of sofpironium and BBI-4010 were less than 0.5% of the applied dose.5
- Half-life
The in vitro half-life sofpironium in human plasma has been measured at 3.86 hours.6
- Clearance
Not Available
- 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
In the event of an overdose via overapplication of sofpironium bromide topical gel, prescribing information recommends washing the area with soap and water.5 Patients experiencing an overdose are likely to exhibit anticholinergic toxicities, including mydriasis (pupil dilation), blurred vision, urinary retention, and temperature dysregulation. Symptoms attributed to sofpironium overdose should be treated symptomatically.5
- 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 softwareAclidinium Sofpironium may increase the anticholinergic activities of Aclidinium. Amantadine Sofpironium may increase the anticholinergic activities of Amantadine. Amitriptyline Sofpironium may increase the anticholinergic activities of Amitriptyline. Amobarbital Sofpironium may increase the anticholinergic activities of Amobarbital. Amoxapine Sofpironium may increase the anticholinergic activities of Amoxapine. - Food Interactions
- No interactions found.
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 Sofpironium bromide 7B2Y1932XU 1628106-94-4 FIAFMTCUJCWADZ-JOFREBOKSA-M - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Sofdra Gel 87 mg/0.67mL Topical Botanix SB Inc. 2024-08-06 Not applicable US
Categories
- Drug Categories
- Anticholinergic Agents
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- MATE 1 Inhibitors
- MATE inhibitors
- Muscarinic Antagonists
- OCT1 inhibitors
- OCT2 Inhibitors
- Classification
- Not classified
- Affected organisms
- Humans
Chemical Identifiers
- UNII
- 00Y6A5AJU6
- CAS number
- 1628251-49-9
- InChI Key
- SEVCTUCCZYBJER-BSJAROSPSA-N
- InChI
- InChI=1S/C22H32NO5/c1-3-27-20(24)16-23(2)14-13-19(15-23)28-21(25)22(26,18-11-7-8-12-18)17-9-5-4-6-10-17/h4-6,9-10,18-19,26H,3,7-8,11-16H2,1-2H3/q+1/t19-,22-,23?/m1/s1
- IUPAC Name
- SMILES
- CCOC(=O)C[N+]1(C)CC[C@H](C1)OC(=O)[C@@](O)(C1CCCC1)C1=CC=CC=C1
References
- Synthesis Reference
Marubayashi K, Watanabe M, & Brinkman HR. (2021). Crystalline form of sofpironium bromide and preparation method thereof. (US Patent No. US11584715B2). U.S. Patent and Trademark Office.
- General References
- Yokozeki H, Fujimoto T, Abe Y, Igarashi M, Ishikoh A, Omi T, Kanda H, Kitahara H, Kinoshita M, Nakasu I, Hattori N, Horiuchi Y, Maruyama R, Mizutani H, Murakami Y, Watanabe C, Kume A, Hanafusa T, Hamaguchi M, Yoshioka A, Egami Y, Matsuo K, Matsuda T, Akamatsu M, Yorozuya T, Takayama S: A phase 3, multicenter, randomized, double-blind, vehicle-controlled, parallel-group study of 5% sofpironium bromide (BBI-4000) gel in Japanese patients with primary axillary hyperhidrosis. J Dermatol. 2021 Mar;48(3):279-288. doi: 10.1111/1346-8138.15668. Epub 2021 Jan 7. [Article]
- Armstrong A, Reddy R, Chadha D, Kircik L: SUPPLEMENT ARTICLE: A Novel Drug Delivery Method: Retrometabolic Drug Design. J Drugs Dermatol. 2022 Apr 1;21(4):s5-s10. [Article]
- Samir A, Ohura K, Bodor N, Imai T: Identification of Major Esterase Involved in Hydrolysis of Soft Anticholinergic (2R3'R-SGM) Designed From Glycopyrrolate in Human and Rat Tissues. J Pharm Sci. 2019 Aug;108(8):2791-2797. doi: 10.1016/j.xphs.2019.03.030. Epub 2019 Apr 5. [Article]
- Dermatology Times: FDA Approves Sofpironium (Sofdra) as First and Only Chemical Entity for Primary Axillary Hyperhidrosis [Link]
- FDA Approved Drug Products: Sofdra (sofpironium bromide) topical gel [Link]
- 2021 Fall Clinical Dermatology Conference: Investigating Treatment of Primary Axillary Hyperhidrosis With a Topical Retrometabolic Anticholinergic Drug [Link]
- External Links
- 2689322
- ChEMBL
- CHEMBL3707224
- Wikipedia
- Sofpironium_bromide
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample data3 Completed Treatment Axillary Hyperhidrosis 2 somestatus stop reason just information to hide 3 Completed Treatment Primary Axillary Hyperhidrosis 1 somestatus stop reason just information to hide 2 Completed Treatment Hyperhidrosis 3 somestatus stop reason just information to hide 2 Completed Treatment Primary Axillary Hyperhidrosis 1 somestatus stop reason just information to hide 1 Completed Treatment Hyperhidrosis 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Gel Topical 87 mg/0.67mL - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Freely soluble https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/217347s000lbl.pdf - Predicted Properties
Property Value Source - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
![](/assets/locked/DrugTargets2-1d1d534575da54e734c316d80c9fb35f8210c070dca913c026f8e58660e3e71a.png)
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover
- Specific Function
- Acetylcholine binding
- Gene Name
- CHRM3
- Uniprot ID
- P20309
- Uniprot Name
- Muscarinic acetylcholine receptor M3
- Molecular Weight
- 66127.445 Da
References
- Yokozeki H, Fujimoto T, Abe Y, Igarashi M, Ishikoh A, Omi T, Kanda H, Kitahara H, Kinoshita M, Nakasu I, Hattori N, Horiuchi Y, Maruyama R, Mizutani H, Murakami Y, Watanabe C, Kume A, Hanafusa T, Hamaguchi M, Yoshioka A, Egami Y, Matsuo K, Matsuda T, Akamatsu M, Yorozuya T, Takayama S: A phase 3, multicenter, randomized, double-blind, vehicle-controlled, parallel-group study of 5% sofpironium bromide (BBI-4000) gel in Japanese patients with primary axillary hyperhidrosis. J Dermatol. 2021 Mar;48(3):279-288. doi: 10.1111/1346-8138.15668. Epub 2021 Jan 7. [Article]
- FDA Approved Drug Products: Sofdra (sofpironium bromide) topical gel [Link]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover
- Specific Function
- G protein-coupled acetylcholine receptor activity
Components:
References
- FDA Approved Drug Products: Sofdra (sofpironium bromide) topical gel [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of fatty acids, steroids and retinoids (PubMed:18698000, PubMed:19965576, PubMed:20972997, PubMed:21289075, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:18698000, PubMed:19965576, PubMed:20972997, PubMed:21289075, PubMed:21576599). Catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) (PubMed:19965576, PubMed:20972997). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 20-hydroxyeicosatetraenoic acid ethanolamide (20-HETE-EA) and 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:18698000, PubMed:21289075). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). Catalyzes the oxidative transformations of all-trans retinol to all-trans retinal, a precursor for the active form all-trans-retinoic acid (PubMed:10681376). Also involved in the oxidative metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants
- Specific Function
- Anandamide 11,12 epoxidase activity
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- FDA Approved Drug Products: Sofdra (sofpironium bromide) topical gel [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of sterols, steroid hormones, retinoids and fatty acids (PubMed:10681376, PubMed:11093772, PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:19965576, PubMed:20702771, PubMed:21490593, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:21490593, PubMed:21576599, PubMed:2732228). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2, as well as D-ring hydroxylated E1 and E2 at the C-16 position (PubMed:11555828, PubMed:12865317, PubMed:14559847). Plays a role in the metabolism of androgens, particularly in oxidative deactivation of testosterone (PubMed:15373842, PubMed:15764715, PubMed:22773874, PubMed:2732228). Metabolizes testosterone to less biologically active 2beta- and 6beta-hydroxytestosterones (PubMed:15373842, PubMed:15764715, PubMed:2732228). Contributes to the formation of hydroxycholesterols (oxysterols), particularly A-ring hydroxylated cholesterol at the C-4beta position, and side chain hydroxylated cholesterol at the C-25 position, likely contributing to cholesterol degradation and bile acid biosynthesis (PubMed:21576599). Catalyzes bisallylic hydroxylation of polyunsaturated fatty acids (PUFA) (PubMed:9435160). Catalyzes the epoxidation of double bonds of PUFA with a preference for the last double bond (PubMed:19965576). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:20702771). Plays a role in the metabolism of retinoids. Displays high catalytic activity for oxidation of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes atRA toward 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Responsible for oxidative metabolism of xenobiotics. Acts as a 2-exo-monooxygenase for plant lipid 1,8-cineole (eucalyptol) (PubMed:11159812). Metabolizes the majority of the administered drugs. Catalyzes sulfoxidation of the anthelmintics albendazole and fenbendazole (PubMed:10759686). Hydroxylates antimalarial drug quinine (PubMed:8968357). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850). Also involved in vitamin D catabolism and calcium homeostasis. Catalyzes the inactivation of the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:29461981)
- Specific Function
- 1,8-cineole 2-exo-monooxygenase activity
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- FDA Approved Drug Products: Sofdra (sofpironium bromide) topical gel [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Electrogenic voltage-dependent transporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics (PubMed:11388889, PubMed:11408531, PubMed:12439218, PubMed:12719534, PubMed:15389554, PubMed:16263091, PubMed:16272756, PubMed:16581093, PubMed:19536068, PubMed:21128598, PubMed:23680637, PubMed:24961373, PubMed:34040533, PubMed:9187257, PubMed:9260930, PubMed:9655880). Functions as a pH- and Na(+)-independent, bidirectional transporter (By similarity). Cation cellular uptake or release is driven by the electrochemical potential (i.e. membrane potential and concentration gradient) and substrate selectivity (By similarity). Hydrophobicity is a major requirement for recognition in polyvalent substrates and inhibitors (By similarity). Primarily expressed at the basolateral membrane of hepatocytes and proximal tubules and involved in the uptake and disposition of cationic compounds by hepatic and renal clearance from the blood flow (By similarity). Most likely functions as an uptake carrier in enterocytes contributing to the intestinal elimination of organic cations from the systemic circulation (PubMed:16263091). Transports endogenous monoamines such as N-1-methylnicotinamide (NMN), guanidine, histamine, neurotransmitters dopamine, serotonin and adrenaline (PubMed:12439218, PubMed:24961373, PubMed:35469921, PubMed:9260930). Also transports natural polyamines such as spermidine, agmatine and putrescine at low affinity, but relatively high turnover (PubMed:21128598). Involved in the hepatic uptake of vitamin B1/thiamine, hence regulating hepatic lipid and energy metabolism (PubMed:24961373). Mediates the bidirectional transport of acetylcholine (ACh) at the apical membrane of ciliated cell in airway epithelium, thereby playing a role in luminal release of ACh from bronchial epithelium (PubMed:15817714). Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with lower efficency (PubMed:17460754). Also capable of transporting non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) (PubMed:11907186). May contribute to the transport of cationic compounds in testes across the blood-testis-barrier (Probable). Also involved in the uptake of xenobiotics tributylmethylammonium (TBuMA), quinidine, N-methyl-quinine (NMQ), N-methyl-quinidine (NMQD) N-(4,4-azo-n-pentyl)-quinuclidine (APQ), azidoprocainamide methoiodide (AMP), N-(4,4-azo-n-pentyl)-21-deoxyajmalinium (APDA) and 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) (PubMed:11408531, PubMed:15389554, PubMed:35469921, PubMed:9260930)
- Specific Function
- (r)-carnitine transmembrane transporter activity
- Gene Name
- SLC22A1
- Uniprot ID
- O15245
- Uniprot Name
- Solute carrier family 22 member 1
- Molecular Weight
- 61153.345 Da
References
- FDA Approved Drug Products: Sofdra (sofpironium bromide) topical gel [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Electrogenic voltage-dependent transporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics (PubMed:9260930, PubMed:9687576). Functions as a Na(+)-independent, bidirectional uniporter (PubMed:21128598, PubMed:9687576). Cation cellular uptake or release is driven by the electrochemical potential, i.e. membrane potential and concentration gradient (PubMed:15212162, PubMed:9260930, PubMed:9687576). However, may also engage electroneutral cation exchange when saturating concentrations of cation substrates are reached (By similarity). Predominantly expressed at the basolateral membrane of hepatocytes and proximal tubules and involved in the uptake and disposition of cationic compounds by hepatic and renal clearance from the blood flow (PubMed:15783073). Implicated in monoamine neurotransmitters uptake such as histamine, dopamine, adrenaline/epinephrine, noradrenaline/norepinephrine, serotonin and tyramine, thereby supporting a physiological role in the central nervous system by regulating interstitial concentrations of neurotransmitters (PubMed:16581093, PubMed:17460754, PubMed:9687576). Also capable of transporting dopaminergic neuromodulators cyclo(his-pro), salsolinol and N-methyl-salsolinol, thereby involved in the maintenance of dopaminergic cell integrity in the central nervous system (PubMed:17460754). Mediates the bidirectional transport of acetylcholine (ACh) at the apical membrane of ciliated cell in airway epithelium, thereby playing a role in luminal release of ACh from bronchial epithelium (PubMed:15817714). Also transports guanidine and endogenous monoamines such as vitamin B1/thiamine, creatinine and N-1-methylnicotinamide (NMN) (PubMed:12089365, PubMed:15212162, PubMed:17072098, PubMed:24961373, PubMed:9260930). Mediates the uptake and efflux of quaternary ammonium compound choline (PubMed:9260930). Mediates the bidirectional transport of polyamine agmatine and the uptake of polyamines putrescine and spermidine (PubMed:12538837, PubMed:21128598). Able to transport non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) (PubMed:11907186). Also involved in the uptake of xenobiotic 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) (PubMed:12395288, PubMed:16394027). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
- Specific Function
- Acetylcholine transmembrane transporter activity
- Gene Name
- SLC22A2
- Uniprot ID
- O15244
- Uniprot Name
- Solute carrier family 22 member 2
- Molecular Weight
- 62579.99 Da
References
- FDA Approved Drug Products: Sofdra (sofpironium bromide) topical gel [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Multidrug efflux pump that functions as a H(+)/organic cation antiporter (PubMed:16330770, PubMed:17509534). Plays a physiological role in the excretion of cationic compounds including endogenous metabolites, drugs, toxins through the kidney and liver, into urine and bile respectively (PubMed:16330770, PubMed:17495125, PubMed:17509534, PubMed:17582384, PubMed:18305230, PubMed:19158817, PubMed:21128598, PubMed:24961373). Mediates the efflux of endogenous compounds such as creatinine, vitamin B1/thiamine, agmatine and estrone-3-sulfate (PubMed:16330770, PubMed:17495125, PubMed:17509534, PubMed:17582384, PubMed:18305230, PubMed:19158817, PubMed:21128598, PubMed:24961373). May also contribute to regulate the transport of cationic compounds in testis across the blood-testis-barrier (Probable)
- Specific Function
- Antiporter activity
- Gene Name
- SLC47A1
- Uniprot ID
- Q96FL8
- Uniprot Name
- Multidrug and toxin extrusion protein 1
- Molecular Weight
- 61921.585 Da
References
- FDA Approved Drug Products: Sofdra (sofpironium bromide) topical gel [Link]
Drug created at August 12, 2024 18:33 / Updated at September 11, 2024 23:10