Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00065)
Name
Betaxolol
Synonyms    Click to Show/Hide the Synonyms of This API
betaxolol; 63659-18-7; Betoptic; Kerlone; Betaxololum; Betaxololum [INN-Latin]; SL 75212; Dextrobetaxolol; 1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-(propan-2-ylamino)propan-2-ol; 1-(4-(2-(Cyclopropylmethoxy)ethyl)phenoxy)-3-((1-methylethyl)amino)-2-propanol; ALO-1401-02; 2-Propanol, 1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-((1-methylethyl)amino)-; CHEBI:3082; (R)-Betaxolol; (+)-Betaxolol; KERLEDEX; NCGC00015159-06; 1-(isopropylamino)-3-[p-(cyclopropylmethoxyethyl)phenoxy]-2-propanol; DSSTox_CID_2674; Betaxolol [INN:BAN]; DSSTox_RID_76685; DSSTox_GSID_22674; C18H29NO3; Betaxolol S; 1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-(isopropylamino)propan-2-ol; 1-{4-[2-(cyclopropylmethoxy)ethyl]phenoxy}-3-(propan-2-ylamino)propan-2-ol; Betaxolol (INN); Betaxolol (TN); CAS-63659-18-7; (S)-Betaxolol hydrochloride;AL-1577A; SL-75212-10; beta-Xolol; Betaxolol (Betoptic); Prestwick0_000382; Prestwick1_000382; Prestwick2_000382; Prestwick3_000382; CHEMBL423; Lopac0_000193; SCHEMBL23530; BSPBio_000563; GTPL549; SPBio_002484; BPBio1_000621; DTXSID2022674; ALO-140102 FREE BASE; HMS2089I07; HMS3655P17; HMS3884L05; HY-B0381; SL-7521210 FREE BASE; Tox21_110091; BDBM50405521; KM0772; AKOS015841671; Tox21_110091_1; AC-1115; CCG-204288; DB00195; SDCCGSBI-0050181.P002; 1-[(4-{2-[(cyclopropylmethyl)oxy]ethyl}phenyl)oxy]-3-[(1-methylethyl)amino]propan-2-ol; MRF-0000336; NCGC00015159-04; NCGC00015159-05; NCGC00015159-08; NCGC00015159-09; NCGC00015159-11; NCGC00015159-13; NCGC00015159-14; NCGC00015159-23; NCGC00024863-03; NCGC00024863-04; AK546815; AS-14125; FT-0773524; SW196917-5; C06849; D07526; 659X187; A834454; L000125; Q794162; Q-200713; BRD-A02759312-003-03-9; BRD-A02759312-003-11-2; (.+/-.)-1-[p-[2-(Cyclopropylmethoxy)ethyl]phenoxy]-3-(isopropylamino)-2-propanol; 1-(4-[2-(Cyclopropylmethoxy)ethyl]phenoxy)-3-(isopropylamino)-2-propanol #; 1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-(propan-2-ylamino)-2-propanol
Clinical Status
Approved
Disease Indication Essential hypertension ICD-11: BA00 [1]
PubChem CID
2369
Formula
C18H29NO3
Canonical SMILES
CC(C)NCC(COC1=CC=C(C=C1)CCOCC2CC2)O
InChI
1S/C18H29NO3/c1-14(2)19-11-17(20)13-22-18-7-5-15(6-8-18)9-10-21-12-16-3-4-16/h5-8,14,16-17,19-20H,3-4,9-13H2,1-2H3
InChIKey
NWIUTZDMDHAVTP-UHFFFAOYSA-N
   Click to Show/Hide the Molecular Data (Structure/Property) of This API
Structure
<iframe style="width: 300px; height: 300px;" frameborder="0" src="https://embed.molview.org/v1/?mode=balls&cid=2369"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 307.4 Topological Polar Surface Area 50.7
XlogP 2.8 Complexity 286
Heavy Atom Count 22 Rotatable Bond Count 11
Hydrogen Bond Donor Count 2 Hydrogen Bond Acceptor Count 4
Full List of Drug Formulations (DFMs) Containing This API
          Betaxolol 10 mg tablet Click to Show/Hide the Full List of Formulation(s):          6 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Stearic acid; Anhydrous lactose; Titanium dioxide; Polyethylene glycol 400; Polysorbate 80; Cellulose, microcrystalline; Hypromellose 2910 (6 mpa.s); Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company KVK Tech
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [3]
             Drug Formulation 2 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Stearic acid; Anhydrous lactose; Titanium dioxide; Polysorbate 80; Carnauba wax; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycol; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company Golden State Medical Supply
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
             Drug Formulation 3 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Stearic acid; Anhydrous lactose; Titanium dioxide; Polysorbate 80; Carnauba wax; Cellulose, microcrystalline; Hypromellose 2208 (100 mpa.s); Polyethylene glycols; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company Epic Pharma; PuraCap Laboratories
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
             Drug Formulation 4 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Stearic acid; Anhydrous lactose; Titanium dioxide; Polysorbate 80; Carnauba wax; Cellulose, microcrystalline; Hypromellose 2208 (100 mpa.s); Polyethylene glycols; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company Marlex Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
             Drug Formulation 5 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Stearic acid; Anhydrous lactose; Titanium dioxide; Polysorbate 80; Carnauba wax; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company Physicians Total Care
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
             Drug Formulation 6 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose; Magnesium stearate; Titanium dioxide; Hydroxypropyl methylcellulose; Polyethylene glycol 400; Colloidal silicon dioxide; Microcrystalline cellulose; Sodium starch glycolate
                   Dosage Form Oral Tablet
                   Company Sanofi-Aventis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [8]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [3]
          Betaxolol 20 mg tablet Click to Show/Hide the Full List of Formulation(s):          4 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Stearic acid; Anhydrous lactose; Titanium dioxide; Polyethylene glycol 400; Polysorbate 80; Cellulose, microcrystalline; Hypromellose 2910 (6 mpa.s); Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company KVK Tech
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [3]
             Drug Formulation 2 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Stearic acid; Anhydrous lactose; Titanium dioxide; Polysorbate 80; Carnauba wax; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycol; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company Golden State Medical Supply
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
             Drug Formulation 3 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Stearic acid; Anhydrous lactose; Titanium dioxide; Polysorbate 80; Carnauba wax; Cellulose, microcrystalline; Hypromellose 2208 (100 mpa.s); Polyethylene glycols; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company Epic Pharma; Marlex Pharmaceuticals; PuraCap Laboratories
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
             Drug Formulation 4 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose; Magnesium stearate; Titanium dioxide; Hydroxypropyl methylcellulose; Polyethylene glycol 400; Colloidal silicon dioxide; Microcrystalline cellulose; Sodium starch glycolate
                   Dosage Form Oral Tablet
                   Company Sanofi-Aventis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [8]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [3]
          Betaxolol Hydrochloride eq 0.25% base suspension Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Benzalkonium Chloride; Mannitol; Poly Sulfonic Acid; Carbomer 934P; Edetate Disodium; Hydrochloric Acid; Sodium Hydroxide; Purified Water
                   Dosage Form Suspension
                   Company Novartis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Acrylic acid DIG Info Choline acetylase (IC50 < 200000 nM) [5]
Hydrochloric acid DIG Info Carbonic anhydrase V (Ki = 156 nM) [6]
Benzalkonium chloride DIG Info Solute carrier SLCO2B1 (Ki = 62.1 uM) [7]
          Betaxolol Hydrochloride 10mg tablet Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Hydroxypropyl Methylcellulose; Lactose; Magnesium Stearate; Polyethylene Glycol 400; Microcrystalline Cellulose; Colloidal Silicon Dioxide; Sodium Starch Glycolate; Titanium Dioxide
                   Dosage Form Tablet
                   Company Sanofi Aventis Us
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [8]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [3]
          Betaxolol Hydrochloride eq 0.5% base solution Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Benzalkonium Chloride; Edetate Disodium; Sodium Chloride; Hydrochloric Acid; Sodium Hydroxide; Purified Water
                   Dosage Form Solution
                   Company Sandoz
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Hydrochloric acid DIG Info Carbonic anhydrase V (Ki = 156 nM) [6]
Benzalkonium chloride DIG Info Solute carrier SLCO2B1 (Ki = 62.1 uM) [7]
References
1 FDA label for approved betaxolol from the official website of the U.S. Food and Drug Administration.
2 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
3 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
4 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.
5 Chemistry and biological activities of N,N-dimethylaminoethyl acrylate, a choline acetyltransferase inhibitor. J Med Chem. 1976 Feb; 19(2):300-3.
6 Carbonic anhydrase inhibitors. Inhibition of the newly isolated murine isozyme XIII with anions. Bioorg Med Chem Lett. 2004 Nov 1; 14(21):5435-9.
7 Bacterial metabolism rescues the inhibition of intestinal drug absorption by food and drug additives. Proc Natl Acad Sci U S A. 2020 Jul 7;117(27):16009-16018.
8 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
9 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.

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