Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00584)
Name
Ranolazine
Synonyms    Click to Show/Hide the Synonyms of This API
RANOLAZINE; 95635-55-5; Ranexa; CVT-303; Ranolazine (Ranexa); RS-43285-003; 142387-99-3; CHEBI:87690; C24H33N3O4; CVT 303; NCGC00015897-02; DSSTox_CID_25196; DSSTox_RID_80743; DSSTox_GSID_45196; (-)-Ranolazine; Latixa; (+-)-Ranolazine; CAS-95635-55-5; Ranexa (TN); SR-01000076216; Ranolazine (USAN/INN); Ranolazine [USAN:INN:BAN]; HSDB 7924; KEG-1295; (+/-)-Ranolazine; CHEMBL1404; Lopac0_001062; BSPBio_002276; MLS002154149; SCHEMBL124665; SPECTRUM1505366; GTPL7291; DTXSID3045196; HMS1922F16; HMS2090L09; HMS2093D21; HMS2098K06; HMS2230C19; HMS3369I08; HMS3655M12; HMS3715K06; HMS3884I10; Pharmakon1600-01505366; ACT06286; BCP04190; HY-B0280; Tox21_110258; BDBM50173335; CR0012; MFCD00864690; NSC759100; NSC782305; AKOS015889500; Tox21_110258_1; AC-1673; BCP9000558; CCG-205139; DB00243; KS-1244; MCULE-8182023610; NSC-759100; NSC-782305; PB21724; SB13209; SDCCGSBI-0051032.P003; NCGC00015897-03; NCGC00015897-04; NCGC00015897-05; NCGC00015897-06; NCGC00015897-08; NCGC00015897-22; NCGC00095177-01; NCGC00095177-02; NCGC00095177-03; 110445-25-5; AK-72950; BR-72950; SMR000857382; BCP0726000090; SBI-0051032.P002; AB0007809; FT-0601594; FT-0674327; SW197620-4; D05700; RS 43285-003; S-1794; AB00698532-11; AB00698532-13; AB00698532-14; AB00698532-15; AB00698532_16; AB00698532_17; AB00698532_18; 635R555; Q907104; SR-01000076216-5; SR-01000076216-8; BRD-A97674275-001-01-9; BRD-A97674275-001-04-3; Z68563450; (+/-)-4-(2-Hydroxy-3-(o-methoxyphenoxy)propyl)-1-piperazineaceto-2',6'-xylidide; 1080496-58-7
Clinical Status
Approved
Disease Indication Angina pectoris ICD-11: BA40 [1]
PubChem CID
56959
Formula
C24H33N3O4
Canonical SMILES
CC1=C(C(=CC=C1)C)NC(=O)CN2CCN(CC2)CC(COC3=CC=CC=C3OC)O
InChI
1S/C24H33N3O4/c1-18-7-6-8-19(2)24(18)25-23(29)16-27-13-11-26(12-14-27)15-20(28)17-31-22-10-5-4-9-21(22)30-3/h4-10,20,28H,11-17H2,1-3H3,(H,25,29)
InChIKey
XKLMZUWKNUAPSZ-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=56959"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 427.5 Topological Polar Surface Area 74.3
XlogP 2.7 Complexity 531
Heavy Atom Count 31 Rotatable Bond Count 9
Hydrogen Bond Donor Count 2 Hydrogen Bond Acceptor Count 6
Full List of Drug Formulations (DFMs) Containing This API
          Ranolazine 500 mg tablet Click to Show/Hide the Full List of Formulation(s):          3 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 yellow no. 6; Magnesium stearate; Sodium hydroxide; Titanium dioxide; Polyethylene glycol 400; Polysorbate 80; Aluminum oxide; Carnauba wax; Cellulose, microcrystalline; Hypromellose 2910 (3 cps); Hypromellose 2910 (5 cps); Hypromellose 2910 (6 cps); Methacrylic acid - ethyl acrylate copolymer (1:1) type a
                   Dosage Form 12 HR Extended Release Oral Tablet
                   Company Gilead Sciences
                   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]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
             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; Ferric oxide red; Ferric oxide yellow; Sodium hydroxide; Talc; Titanium dioxide; Water; Polyethylene glycol 3350; Polyvinyl alcohol; Carnauba wax; Cellulose, microcrystalline; Hypromelloses; Methacrylic acid - ethyl acrylate copolymer (1:1) type a
                   Dosage Form 12 HR Extended Release Oral Tablet
                   Company Aphena Pharma Solutions-Tennessee; Cardinal Health; Carilion Materials Management; Gilead Sciences
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [6]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 3350 DIG Info Albendazole monooxygenase (Protein expression upregulation) [4]
             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; Ferric oxide red; Ferric oxide yellow; Sodium hydroxide; Talc; Titanium dioxide; Polyethylene glycol 400; Polyvinyl alcohol; Carnauba wax; Cellulose, microcrystalline; Hypromellose 2910 (5 mpa.s); Methacrylic acid - ethyl acrylate copolymer (1:1) type a
                   Dosage Form 12 HR Extended Release Oral Tablet
                   Company Cardinal Health
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [6]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
          Ranolazine 1000 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
Lactose monohydrate; Magnesium stearate; Ferric oxide yellow; Sodium hydroxide; Titanium dioxide; Triacetin; Water; Polyethylene glycol 3350; Carnauba wax; Cellulose, microcrystalline; Hypromellose 2910 (6 mpa.s); Hypromelloses; Methacrylic acid - ethyl acrylate copolymer (1:1) type a
                   Dosage Form 12 HR Extended Release Oral Tablet
                   Company Gilead Sciences
                   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) [4]
Polyethylene glycol 3350 DIG Info Albendazole monooxygenase (Protein expression upregulation) [4]
             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; Magnesium stearate; Ferric oxide yellow; Sodium hydroxide; Titanium dioxide; Triacetin; Polyethylene glycol 3350; Carnauba wax; Cellulose, microcrystalline; Hypromellose 2910 (5 cps); Hypromellose 2910 (6 cps); Methacrylic acid - ethyl acrylate copolymer (1:1) type a
                   Dosage Form 12 HR Extended Release Oral Tablet
                   Company Gilead Sciences
                   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) [4]
Polyethylene glycol 3350 DIG Info Albendazole monooxygenase (Protein expression upregulation) [4]
References
1 FDA label for approved ranolazine 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 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
4 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
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 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.

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