Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00672)
Name
Thioridazine
Synonyms    Click to Show/Hide the Synonyms of This API
thioridazine; Mellaril; 50-52-2; Thioridazin; Melleril; Meleril; Malloryl; Sonapax; Mellaril-S; Mallorol; Mellerets; Mellerette; Melleretten; dl-Thioridazine; Tioridazina; Melleril (liquid); Thioridazinum; 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine; Orsanil; 2-Methylmercapto-10-(2-(N-methyl-2-piperidyl)ethyl)phenothiazine; 3-Methylmercapto-N-(2'-(N-methyl-2-piperidyl)ethyl)phenothiazine; Melleryl; CHEMBL479; 10-(2-(1-Methyl-2-piperidyl)ethyl)-2-(methylthio)phenothiazine; 10-[2-(1-methyl-2-piperidyl)ethyl]-2-methylsulfanyl-phenothiazine; 10-[2-(1-methylpiperidin-2-yl)ethyl]-2-methylsulfanylphenothiazine; 10-[2-(1-methylpiperidin-2-yl)ethyl]-2-(methylsulfanyl)-10H-phenothiazine; 10H-Phenothiazine, 10-(2-(1-methyl-2-piperidinyl)ethyl)-2-(methylthio)-; CHEBI:9566; NCGC00016059-05; (+-)-Thioridazine; Mellarit; Thiozine; Malloryl; Meleril; Mellaril S; Mellerets; Phenothiazine, 10-((1-methyl-2-piperidyl)ethyl)-2-(methylthio)-; Thioridazine prolongatum; DSSTox_CID_3656; 10H-Phenothiazine, 10-[2-(1-methyl-2-piperidinyl)ethyl]-2-(methylthio)-; DSSTox_RID_77130; DSSTox_GSID_23656; Thioridazinum [INN-Latin]; Tioridazina [INN-Spanish]; Thioxidazine; Thioridazine, prolongatum; Phenothiazine, 10-[2-(1-methyl-2-piperidyl)ethyl]-2-(methylthio)-; 10-[2-(1-methylpiperidin-2-yl)ethyl]-2-(methylthio)-10H-phenothiazine; CAS-50-52-2; Mellaril-S (TN); NSC186060; HSDB 3189; C21H26N2S2; EINECS 200-044-2; Thioridazine (USP/INN); Mellaril (*Hydrochloride*); AI3-51923; Thioridazine [USAN:USP:INN:BAN]; Mellaril (Salt/Mix); Spectrum_001066; Prestwick0_000078; Prestwick1_000078; Prestwick2_000078; Prestwick3_000078; Spectrum2_001332; Spectrum3_000585; Spectrum4_000356; Spectrum5_001062; (.+/-.)-Thioridazine; Biomol-NT_000017; SCHEMBL9566; Lopac0_001252; BSPBio_000295; BSPBio_002030; GTPL100; KBioGR_000791; KBioGR_002308; KBioSS_001546; KBioSS_002310; DivK1c_000066; SPBio_001483; SPBio_002216; BPBio1_000325; BPBio1_001175; DTXSID6023656; SCHEMBL12434241; KBio1_000066; KBio2_001546; KBio2_002308; KBio2_004114; KBio2_004876; KBio2_006682; KBio2_007444; KBio3_001530; KBio3_002788; cMAP_000015; NINDS_000066; HMS2090J04; BCP19922; Tox21_110294; 6960AB; BDBM50002338; NS-835; 10-[2-(1-Methyl-2-piperidinyl)ethyl]-2-(methylsulfanyl)-10H-phenothiazine; Tox21_110294_1; CCG-205326; DB00679; MCULE-7796139302; SDCCGSBI-0051219.P005; IDI1_000066; NCGC00016059-03; NCGC00016059-04; NCGC00016059-07; NCGC00016059-08; NCGC00016059-09; NCGC00016059-10; NCGC00016059-11; NCGC00016059-13; NCGC00016059-14; NCGC00016059-24; NCGC00089809-02; NCGC00089809-03; SBI-0051219.P004; AB00053553; 1452-EP2272537A2; 1452-EP2275420A1; 1452-EP2298776A1; D00373; Q58375; AB00053553-16; AB00053553_17; AB00053553_18; 242T875; L001321; BRD-A84481105-003-17-2; 10-[2-(1-methyl-piperidin-2-yl)-ethyl]-2-methylsulfanyl-10h-phenothiazine; 10H-Phenothiazine, 10-[2-(1-methyl-2-piperidyl)ethyl]-2-methylthio-; 10-[2-(1-Methyl-2-piperidinyl)ethyl]-2-(methylsulfanyl)-10H-phenothiazine #; 107388-89-6
Clinical Status
Approved
Disease Indication Schizophrenia ICD-11: 6A20 [1]
PubChem CID
5452
Formula
C21H26N2S2
Canonical SMILES
CN1CCCCC1CCN2C3=CC=CC=C3SC4=C2C=C(C=C4)SC
InChI
1S/C21H26N2S2/c1-22-13-6-5-7-16(22)12-14-23-18-8-3-4-9-20(18)25-21-11-10-17(24-2)15-19(21)23/h3-4,8-11,15-16H,5-7,12-14H2,1-2H3
InChIKey
KLBQZWRITKRQQV-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=5452"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 370.6 Topological Polar Surface Area 57.1
XlogP 5.9 Complexity 432
Heavy Atom Count 25 Rotatable Bond Count 4
Hydrogen Bond Donor Count 0 Hydrogen Bond Acceptor Count 4
Full List of Drug Formulations (DFMs) Containing This API
          Thioridazine 10 mg 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
Sodium lauryl sulfate; Fd&c yellow no. 6; Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Silicon dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose (type h); Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Mylan Pharamceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
          Thioridazine 100 mg 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
Sodium lauryl sulfate; Fd&c yellow no. 6; Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Silicon dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose (type h); Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Mylan Pharamceuticals; RemedyRepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
          Thioridazine 25 mg tablet Click to Show/Hide the Full List of Formulation(s):          2 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
Sodium lauryl sulfate; Fd&c yellow no. 6; Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Silicon dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose (type h); Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Mylan Pharamceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
Sodium lauryl sulfate; Fd&c yellow no. 6; Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Silicon dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose; Hypromelloses; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company RemedyRepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
          Thioridazine 50 mg tablet Click to Show/Hide the Full List of Formulation(s):          2 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
Sodium lauryl sulfate; Fd&c yellow no. 6; Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Silicon dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose (type h); Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Mylan Pharamceuticals; RemedyRepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
Sodium lauryl sulfate; Fd&c yellow no. 6; Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Silicon dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose; Hypromelloses; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company RemedyRepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
          Thioridazine Hydrochloride 25mg 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
Silicon Dioxide; Croscarmellose Sodium; Fd&C Yellow No. 6; Hydroxypropyl Cellulose, Unspecified; Hypromellose, Unspecified; Magnesium Stearate; Microcrystalline Cellulose; Polyethylene Glycol, Unspecified; Sodium Lauryl Sulfate; Titanium Dioxide
                   Dosage Form Tablet
                   Company Mylan Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [2]
Hydroxypropyl cellulose DIG Info Mephenytoin 4-hydroxylase (EC50 = 89.5 uM) [4]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
          Thioridazine Hydrochloride 100mg 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
Silicon Dioxide; Croscarmellose Sodium; Fd&C Yellow No. 6; Hydroxypropyl Cellulose, Unspecified; Hypromellose, Unspecified; Magnesium Stearate; Microcrystalline Cellulose; Polyethylene Glycol, Unspecified; Sodium Lauryl Sulfate; Titanium Dioxide
                   Dosage Form Tablet
                   Company Remedyrepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [2]
Hydroxypropyl cellulose DIG Info Mephenytoin 4-hydroxylase (EC50 = 89.5 uM) [4]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
References
1 FDA label for approved thioridazine from the official website of the U.S. Food and Drug Administration.
2 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.
3 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
4 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
5 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.

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