Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00579)
Name
Raloxifene
Synonyms    Click to Show/Hide the Synonyms of This API
raloxifene; 84449-90-1; Keoxifene; Evista; Raloxifenum [Latin]; Raloxifeno [Spanish]; Raloxifenum; Raloxifeno; LY 139481; LY-139481; UNII-YX9162EO3I; Optruma; CHEMBL81; Keoxifene; LY 139481;; CHEBI:8772; YX9162EO3I; Raloxifene [INN:BAN]; CCRIS 7129; HSDB 7460; NCGC00015889-05; CAS-82640-04-8; Pharoxifene; Raloxifene, 6; Raloxifene (INN); Eviden (TN); Raxeto (TN); Prestwick0_000862; Prestwick1_000862; Prestwick2_000862; Prestwick3_000862; Lopac-R-1402; DSSTox_CID_3550; SCHEMBL6144; DSSTox_RID_77076; DSSTox_GSID_23550; Lopac0_001051; BSPBio_000903; KBioGR_002361; KBioSS_002364; BIDD:ER0216; BIDD:GT0795; SPBio_002824; BPBio1_000995; GTPL2820; DTXSID3023550; BDBM19441; KBio2_002361; KBio2_004929; KBio2_007497; KBio3_002840; cid_11071264; cMAP_000032; HMS2089F06; HMS3742O11; ZINC538275; BCP09772; Tox21_202603; MFCD00866415; NSC747974; NSC761389; AKOS015896267; AC-8399; CCG-205128; DB00481; MCULE-4598311006; NSC-747974; NSC-761389; SDCCGSBI-0051021.P003; 2-(4-hydroxyphenyl)-3-{4-[2-(piperidin-1-yl)ethoxy]benzoyl}-1-benzothiophen-6-ol; MRF-0000684; SMP2_000095; NCGC00015889-01; NCGC00015889-02; NCGC00015889-04; NCGC00015889-06; NCGC00015889-07; NCGC00015889-08; NCGC00015889-10; NCGC00015889-22; NCGC00092353-02; NCGC00092353-04; NCGC00260151-01; AS-35086; HY-13738; J22.982B; LY139481; SBI-0051021.P002; AB0073011; CAS-84449-90-1; CS-0007764; FT-0674305; VU0155042-3; C07228; D08465; 15189-EP2270008A1; 15189-EP2272825A2; 15189-EP2280012A2; 15189-EP2281815A1; 15189-EP2289892A1; 15189-EP2292615A1; 15189-EP2292617A1; 15189-EP2295426A1; 15189-EP2295427A1; 15189-EP2301928A1; 15189-EP2301933A1; 15189-EP2305640A2; 15189-EP2305671A1; 15189-EP2308855A1; 15189-EP2311808A1; 15189-EP2311825A1; 15189-EP2311827A1; 15189-EP2311829A1; 15189-EP2311840A1; 15189-EP2311842A2; 15189-EP2314581A1; 15189-EP2316832A1; 15189-EP2316833A1; 449R901; Q425223; BRD-K63828191-003-11-5; 6-hydroxy-2-(4-hydoxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene; 6-hydroxy-2-(4-hydoxyphenyl)-3[-4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene; 6-Hydroxy-2-(4-Hydroxyphenyl)-3-[4(2-Piperidinoethoxy)benzoyl]benzo[b]thiophene; 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene; 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2piperidinoethoxy)-benzoyl]benzo[b]thiophene; 6-hydroxy-2-(4-hydroxyphenyl)-3[-4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene; 6-hydroxy-2-(4-hydroxyphenyl)-3[-4-(2piperidinoethoxy)benzoyl]benzo[b]thiophene; 6-hydroxy-2-(4-hyroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene; 1020061-04-4
Clinical Status
Approved
Disease Indication Osteoporosis ICD-11: FB83 [1]
PubChem CID
5035
Formula
C28H27NO4S
Canonical SMILES
C1CCN(CC1)CCOC2=CC=C(C=C2)C(=O)C3=C(SC4=C3C=CC(=C4)O)C5=CC=C(C=C5)O
InChI
1S/C28H27NO4S/c30-21-8-4-20(5-9-21)28-26(24-13-10-22(31)18-25(24)34-28)27(32)19-6-11-23(12-7-19)33-17-16-29-14-2-1-3-15-29/h4-13,18,30-31H,1-3,14-17H2
InChIKey
GZUITABIAKMVPG-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=5035"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 473.6 Topological Polar Surface Area 98.2
XlogP 6.1 Complexity 655
Heavy Atom Count 34 Rotatable Bond Count 7
Hydrogen Bond Donor Count 2 Hydrogen Bond Acceptor Count 6
Full List of Drug Formulations (DFMs) Containing This API
          Raloxifene 60 mg tablet Click to Show/Hide the Full List of Formulation(s):        12 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
Magnesium stearate; Mannitol; Titanium dioxide; Crospovidone; Poloxamer 407; Polyethylene glycol 400; Polysorbate 80; Hydroxypropyl cellulose (type h); Hypromellose 2910 (3 mpa.s); Hypromellose 2910 (6 mpa.s)
                   Dosage Form Oral Tablet
                   Company American Health Packaging; Cipla; Liberty Pharmaceuticals
                   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) [2]
Poloxamer 407 DIG Info Albendazole monooxygenase (EC50 = 32.8 uM) [3]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [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
Magnesium stearate; Mannitol; Titanium dioxide; Crospovidone; Poloxamer 407; Polyethylene glycol 400; Polysorbate 80; Hydroxypropyl cellulose; Hypromellose 2910 (3 mpa.s); Hypromellose 2910 (6 mpa.s)
                   Dosage Form Oral Tablet
                   Company Camber Pharmaceuticals; Exelan Pharmaceuticals
                   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) [2]
Poloxamer 407 DIG Info Albendazole monooxygenase (EC50 = 32.8 uM) [3]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [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
Magnesium stearate; Mannitol; Titanium dioxide; Poloxamer 407; Polyethylene glycol 400; Polysorbate 80; Crospovidone (15 mpa.s at 5%); Hydroxypropyl cellulose (type h); Hypromellose 2910 (3 mpa.s); Hypromellose 2910 (6 mpa.s)
                   Dosage Form Oral Tablet
                   Company American Health Packaging
                   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) [2]
Poloxamer 407 DIG Info Albendazole monooxygenase (EC50 = 32.8 uM) [3]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [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; Sodium stearyl fumarate; Citric acid monohydrate; Titanium dioxide; Polysorbate 80; Silicon dioxide; Hypromelloses; Polyethylene glycols; Starch, corn
                   Dosage Form Oral Tablet
                   Company Actavis Pharma; Avera McKennan Hospital
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
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) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
Anhydrous lactose; Lactose monohydrate; Magnesium stearate; Propylene glycol; Titanium dioxide; Crospovidone; Hypromellose; Polysorbate 80; Povidone; Carnauba wax; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company Physicians Total Care
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [6]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [3]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
Anhydrous lactose; Lactose monohydrate; Magnesium stearate; Propylene glycol; Titanium dioxide; Crospovidone; Polysorbate 80; Povidone; Carnauba wax; Hypromelloses; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company Lake Eire Medical & Surgical Supply DBA Quality Care Products
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [6]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
Anhydrous lactose; Lactose monohydrate; Magnesium stearate; Propylene glycol; Titanium dioxide; Crospovidone; Polysorbate 80; Povidone; Carnauba wax; Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company PD-Rx Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [6]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
Anhydrous lactose; Lactose monohydrate; Magnesium stearate; Titanium dioxide; Crospovidone; Polysorbate 80; Povidone; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Amneal Pharmaceuticals; Avera McKennan Hospital; Kaiser Foundation Hospitals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
Anhydrous lactose; Lactose monohydrate; Magnesium stearate; Talc; Titanium dioxide; Poloxamer 407; Polyethylene glycol 4000; Silicon dioxide; Cellulose, microcrystalline; Crospovidone (15 mpa.s at 5%); Hypromelloses
                   Dosage Form Oral Tablet
                   Company Glenmark Pharmaceutials
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Poloxamer 407 DIG Info Albendazole monooxygenase (EC50 = 32.8 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [6]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
Magnesium stearate; Citric acid monohydrate; Titanium dioxide; Crospovidone; Polyethylene glycol 400; Polysorbate 80; Povidone k30; Cellulose, microcrystalline; Hypromellose 2910 (5 mpa.s)
                   Dosage Form Oral Tablet
                   Company Aphena Pharma Solutions-Tennessee; Aurobindo Pharma; Kaiser Foundation Hospitals; Lucid Pharma; Prasco
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [6]
             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
Magnesium stearate; Titanium dioxide; Polyethylene glycol 4000; Povidone k30; Silicon dioxide; Cellulose, microcrystalline; Hypromellose 2910 (15 mpa.s); Polydextrose; Starch, corn
                   Dosage Form Oral Tablet
                   Company AvKARE; Teva 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) [5]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [6]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             Drug Formulation 12 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
Magnesium stearate; Citric acid monohydrate; Titanium dioxide; Polysorbate 80; Crospovidone, unspecified; Hypromellose, unspecified; Microcrystalline cellulose; Polyethylene glycol, unspecified; Povidone, unspecified
                   Dosage Form Oral Tablet
                   Company Dr Reddy's Laboratories; ScieGen Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
          Raloxifene Hydrochloride 60mg 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
Mannitol; Crospovidone; Hydroxypropyl Cellulose; Poloxamer 407; Magnesium Stearate; Opadry White (Titanium Dioxide; Hypromellose 2910 (3Cp); Hypromellose 2910 (6Cp); Macrogol/Peg 400; Polysorbate 80
                   Dosage Form Tablet
                   Company Aphena Pharma Solutions - Tennessee ; Exelan Pharmaceuticals
                   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) [2]
Hydroxypropyl cellulose DIG Info Mephenytoin 4-hydroxylase (EC50 = 89.5 uM) [3]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [3]
Poloxamer 407 DIG Info Albendazole monooxygenase (EC50 = 32.8 uM) [3]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [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
Colloidal Silicon Dioxide; Hypromellose; Magnesium Stearate; Microcrystalline Cellulose; Polydextrose; Polyethylene Glycol; Povidone; Pregelatinized Starch; Titanium Dioxide
                   Dosage Form Tablet
                   Company Remedyrepack
                   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) [3]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [6]
Pregelatinized starch DIG Info Multidrug resistance protein 1 (Protein expression downregulation) [5]
References
1 FDA label for approved raloxifene from the official website of the U.S. Food and Drug Administration.
2 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.
3 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
4 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
5 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
6 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
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.

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