Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00180)
Name
Desloratadine
Synonyms    Click to Show/Hide the Synonyms of This API
Desloratadine; 100643-71-8; Clarinex; Descarboethoxyloratadine; Desloratidine; Neoclarityn; Sch-34117; Aerius; Azomyr; Denosin; Sch 34117; Descarboethoxyoratidine; UNII-FVF865388R; MFCD00871949; CHEMBL1172; Loratadine related compound a; C19H19ClN2; MLS000559042; CHEBI:291342; FVF865388R; NCGC00159325-02; SMR000149358; Opulis; Clarinex RediTabs; DSSTox_CID_24196; DSSTox_RID_80112; DSSTox_GSID_44196; Desalex; 8-chloro-11-piperidin-4-ylidene-5,6-dihydrobenzo[1,2]cyclohepta[2,4-b]pyridine; Clarinex (TN); CAS-100643-71-8; SR-01000668962; Neoclaritin; Desloratadine [USAN:INN:BAN]; Clarinex(R); MK-4117; CPD000149358; Opera_ID_1891; SCHEMBL4425; MLS000759406; MLS001201801; MLS001424247; BEN691; Desloratadine (JAN/USP/INN); GTPL7157; ZINC1261; DTXSID1044196; Loratadine related compound a rs; HMS2052H05; HMS2090C06; HMS2093F19; HMS3394H05; HMS3652O15; HMS3715J15; HMS3885C18; Pharmakon1600-01505393; ALBB-027276; BCP02340; HY-B0539; Tox21_111574; ANW-42359; BBL010777; BDBM50073179; CD0143; NSC675447; NSC759824; STK586537; AKOS000280921; Tox21_111574_1; AC-1279; CCG-101162; DB00967; KS-1048; MCULE-2975958622; NC00412; NSC-675447; NSC-759824; SB17503; Desloratadine, powder, >=98% (HPLC); NCGC00159325-03; NCGC00159325-04; NCGC00159325-05; AK163520; Loratadine EP Impurity D (Desloratadine); SBI-0206828.P001; AB0012600; FT-0602522; FT-0666048; SW197792-3; A19515; D03693; J10309; AB00456701-11; AB00456701-13; AB00456701_14; AB00456701_15; 643D718; L001025; Q418060; Q-200936; SR-01000668962-4; SR-01000668962-5; SR-01000668962-8; BRD-K82357231-001-13-4; Desloratadine, European Pharmacopoeia (EP) Reference Standard; Desloratadine, United States Pharmacopeia (USP) Reference Standard; Desloratidine, Pharmaceutical Secondary Standard; Certified Reference Material
Clinical Status
Approved
Disease Indication Allergic rhinitis ICD-11: CA08 [1]
PubChem CID
124087
Formula
C19H19ClN2
Canonical SMILES
C1CC2=C(C=CC(=C2)Cl)C(=C3CCNCC3)C4=C1C=CC=N4
InChI
1S/C19H19ClN2/c20-16-5-6-17-15(12-16)4-3-14-2-1-9-22-19(14)18(17)13-7-10-21-11-8-13/h1-2,5-6,9,12,21H,3-4,7-8,10-11H2
InChIKey
JAUOIFJMECXRGI-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=124087"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 310.8 Topological Polar Surface Area 24.9
XlogP 4.5 Complexity 425
Heavy Atom Count 22 Rotatable Bond Count 0
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 2
Full List of Drug Formulations (DFMs) Containing This API
          Desloratadine 5 mg tablet Click to Show/Hide the Full List of Formulation(s):        11 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
Fd&c blue no. 2; Magnesium stearate; Butylated hydroxyanisole; Titanium dioxide; Croscarmellose sodium; Polyethylene glycol 6000; Polysorbate 80; Silicon dioxide; Betadex; Hydroxypropyl cellulose, low substituted; Hypromellose 2910 (6 mpa.s); Starch, corn
                   Dosage Form Oral Tablet
                   Company NorthStar Rx
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Butylhydroxyanisole DIG Info Prostaglandin G/H synthase 2 (IC50 = 2.6 uM) [2]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
Polyethylene glycol 6000 DIG Info Albendazole monooxygenase (Inhibition ratio < 70 %) [4]
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
Anhydrous citric acid; Anhydrous lactose; Sodium stearyl fumarate; Aspartame; Mannitol; Ferric oxide red; Talc; Crospovidone; Silicon dioxide; Cellulose, microcrystalline; Polacrilin
                   Dosage Form Disintegrating Oral Tablet
                   Company Dr Reddy's Laboratories
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [5]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [6]
Aspartame DIG Info Pregnane X receptor (Ki = 13 uM) [2]
Sodium stearyl fumarate DIG Info Leukemia K562 cells (IC50 = 20.2 ug.mL-1) [7]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             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
Sodium lauryl sulfate; Fd&c red no. 40; Magnesium stearate; Talc; Titanium dioxide; Polyvinyl alcohol; Silicon dioxide; Cellulose, microcrystalline; Polyethylene glycols; Starch, corn
                   Dosage Form Oral Tablet
                   Company Mylan Pharamceuticals
                   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]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [8]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [8]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [9]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             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
Sodium stearyl fumarate; Fd&c blue no. 2; Meglumine; Titanium dioxide; Polysorbate 80; Cellulose, microcrystalline; Hypromellose 2910 (15 mpa.s); Polyethylene glycols; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company Sun Pharmaceutical Industries
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Meglumine DIG Info Alglucerase (IC50 = 447000 nM) [10]
Sodium stearyl fumarate DIG Info Leukemia K562 cells (IC50 = 20.2 ug.mL-1) [7]
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
Fd&c blue no. 2; Magnesium hydroxide; Talc; Titanium dioxide; Croscarmellose sodium; Carnauba wax; Cellulose, microcrystalline; Hydroxypropyl cellulose (type h); Hypromelloses; Polyethylene glycols; Starch, corn
                   Dosage Form Oral Tablet
                   Company Paddock Laboratories,
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
             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
Fd&c blue no. 2; Zinc stearate; Talc; Croscarmellose sodium; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Oral Tablet
                   Company AvKARE; AvPAK; Belcher Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
             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
Fd&c blue no. 2; Zinc stearate; Talc; Croscarmellose sodium; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Oral Tablet
                   Company Virtus Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
             Drug Formulation 8 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
Fd&c blue no. 2; Zinc stearate; Talc; Croscarmellose sodium; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Oral Tablet
                   Company Bryant Ranch Prepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
             Drug Formulation 9 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
Fd&c blue no. 2; Titanium dioxide; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols; Starch, corn
                   Dosage Form Oral Tablet
                   Company Sandoz
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             Drug Formulation 10 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; Fd&c blue no. 2; Calcium phosphate, dibasic, dihydrate; Talc; Titanium dioxide; Aluminum oxide; Carnauba wax; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols; Starch, corn; White wax
                   Dosage Form Oral Tablet
                   Company Merck Sharp & Dohme
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
             Drug Formulation 11 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; Fd&c blue no. 2; Dibasic calcium phosphate dihydrate; Talc; Titanium dioxide; Carnauba wax; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycol; Starch, corn; White wax
                   Dosage Form Oral Tablet
                   Company Physicians Total Care
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
          Desloratadine 2.5 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
Anhydrous citric acid; Anhydrous lactose; Sodium stearyl fumarate; Aspartame; Mannitol; Ferric oxide red; Talc; Crospovidone; Silicon dioxide; Cellulose, microcrystalline; Polacrilin
                   Dosage Form Disintegrating Oral Tablet
                   Company Dr Reddy's Laboratories
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [5]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [6]
Aspartame DIG Info Pregnane X receptor (Ki = 13 uM) [2]
Sodium stearyl fumarate DIG Info Leukemia K562 cells (IC50 = 20.2 ug.mL-1) [7]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
References
1 FDA label for approved desloratadine 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 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
4 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
5 PubChem BioAssay data set.
6 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.
7 Synthesis and evaluation of (-)-Massoialactone and analogues as potential anticancer and anti-inflammatory agents. Eur J Med Chem. 2014 Apr 9; 76:291-300.
8 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.
9 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
10 Towards a stable noeuromycin analog with a D-manno configuration: synthesis and glycosidase inhibition of D-manno-like tri- and tetrahydroxylated azepanes. Bioorg Med Chem. 2012 Jan 15; 20(2):641-9.

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