Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00117)
Name
Cevimeline
Synonyms    Click to Show/Hide the Synonyms of This API
Cevimeline; 107233-08-9; Cevimeline HCl; Cevimeline (INN); C10H17NOS; PubChem19118; cevimeline trans-sulfoxide; BIDD:GT0265; SCHEMBL188381; CHEMBL1201267; DTXSID2023777; ZINC10163; AKOS025294043; CS-0397; AS-56166; HY-70020; D07667; W-5959; UNII-K9V0CDQ56E component WUTYZMFRCNBCHQ-PSASIEDQSA-N; (3R,2'R)-2'-Methylspiro[1-azabicyclo[2.2.2]octane-3,5'-[1,3]oxathiolane]
Clinical Status
Approved
Disease Indication Sjogren syndrome ICD-11: 4A43 [1]
PubChem CID
83898
Formula
C10H17NOS
Canonical SMILES
C[C@@H]1O[C@]2(CN3CCC2CC3)CS1
InChI
1S/C10H17NOS/c1-8-12-10(7-13-8)6-11-4-2-9(10)3-5-11/h8-9H,2-7H2,1H3/t8-,10-/m1/s1
InChIKey
WUTYZMFRCNBCHQ-PSASIEDQSA-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=83898"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 199.32 Topological Polar Surface Area 37.8
XlogP 1.5 Complexity 215
Heavy Atom Count 13 Rotatable Bond Count 0
Hydrogen Bond Donor Count 0 Hydrogen Bond Acceptor Count 3
Full List of Drug Formulations (DFMs) Containing This API
          Cevimeline 30 mg capsule Click to Show/Hide the Full List of Formulation(s):          7 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
Lactose monohydrate; D&c yellow no. 10; Fd&c red no. 40; Butyl alcohol; Fd&c yellow no. 6; Isopropyl alcohol; Magnesium stearate; Ammonia; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Gelatin; Hydroxypropyl cellulose (type e); Shellac
                   Dosage Form Oral Capsule
                   Company Novel Laboratories
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 4.7 uM) [2]
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [3]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [2]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [4]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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
Lactose monohydrate; Sodium lauryl sulfate; Magnesium stearate; Ferric oxide red; Glycerin; Titanium dioxide; Water; Hydroxypropyl cellulose (1200000 mw)
                   Dosage Form Oral Capsule
                   Company West-Ward Pharmaceticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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
Lactose monohydrate; Sodium lauryl sulfate; Magnesium stearate; Ferric oxide red; Glycerin; Titanium dioxide; Water; Hydroxypropyl cellulose (type h)
                   Dosage Form Oral Capsule
                   Company Avera McKennan Hospital
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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 monohydrate; Magnesium stearate; Hydroxypropyl cellulose (type h)
                   Dosage Form Oral Capsule
                   Company American Health Packaging
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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
Lactose monohydrate; Magnesium stearate; Hydroxypropyl cellulose, unspecified
                   Dosage Form Oral Capsule
                   Company Ingenus Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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 monohydrate; Magnesium stearate
                   Dosage Form Oral Capsule
                   Company Apotex
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             Drug Formulation 7 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 monohydrate; Magnesium stearate; Hydroxypropyl cellulose
                   Dosage Form Oral Capsule
                   Company Ranbaxy Pharmaceuticals; Stat Rx USA
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
References
1 FDA label for approved cevimeline 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 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.
4 Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. J Med Chem. 2004 Mar 11; 47(6):1413-22.
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.
6 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhang and Dr. Mou.