Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00344)
Name
Ketorolac
Synonyms    Click to Show/Hide the Synonyms of This API
ketorolac; 74103-06-3; 5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid; Ketorolaco; Ketorolacum [Latin]; Ketorolaco [Spanish]; Ketoralac; Ketorolacum; (+-)-Ketorolac; 66635-83-4; rac-ketorolac; RS 37619; Acular; (+)-Ketorolac; (-)-Ketorolac; Toradol (TN); (+-)-5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid; CHEBI:76223; MFCD00864281; RS37619; Macril; 1H-Pyrrolizine-1-carboxylic acid, 2,3-dihydro-5-benzoyl-, (+-)-; 5-(phenylcarbonyl)-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid; Ketorolac [INN:BAN]; RS-37619; (1RS)-5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid; Ketorolac (INN); 1H-Pyrrolizine-1-carboxylic acid, 5-benzoyl-2,3-dihydro-; NCGC00185990-01; CHEMBL469; SCHEMBL14891; MLS006011844; CHEBI:6129; GTPL6661; DTXSID8023189; BDBM85511; HMS3604J05; HMS3884M04; HY-B0580; ABP001024; AC-545; HTS001246; KM1590; STL018674; AKOS005657203; AC-1121; CCG-204762; DB00465; KS-5175; SDCCGSBI-0050655.P004; NCGC00185990-02; NCGC00185990-05; NCGC00185990-15; AK116469; SMR001550090; SY107530; SBI-0050655.P003; AB0008038; CAS_74103-07-4; DB-011403; AB00053682; FT-0653523; FT-0670664; FT-0670665; FT-0670666; C07062; D08104; J10261; AB00053682-12; AB00053682-14; AB00053682_15; AB00053682_16; 635K834; Q2014797; BRD-A40639672-234-05-7; BRD-A40639672-234-09-9; KETOROLAC, ketorolactromethamine, Ketorolac Tromethamine; 5-(benzoyl)-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid; 5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid #; rac-5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid; (.+/-.)-2,3-Dihydro-5-benzoyl-1H-pyrrolizine-1-carboxylic acid; (.+/-.)-5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid; 5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid; 1H-Pyrrolizine-1-carboxylic acid, 2,3-dihydro-5-benzoyl-, (.+/-.)-; 5-BENZOYL-2,3-DIHYDRO-1H-PYRROLO[1,2-A]PYRROLE-1-CARBOXYLIC ACID
Clinical Status
Approved
Disease Indication Rheumatoid arthritis ICD-11: FA20 [1]
PubChem CID
3826
Formula
C15H13NO3
Canonical SMILES
C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O
InChI
1S/C15H13NO3/c17-14(10-4-2-1-3-5-10)13-7-6-12-11(15(18)19)8-9-16(12)13/h1-7,11H,8-9H2,(H,18,19)
InChIKey
OZWKMVRBQXNZKK-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=3826"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 255.27 Topological Polar Surface Area 59.3
XlogP 1.9 Complexity 376
Heavy Atom Count 19 Rotatable Bond Count 3
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 3
Full List of Drug Formulations (DFMs) Containing This API
          Ketorolac 10 mg tablet Click to Show/Hide the Full List of Formulation(s):        13 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 lactose; Sodium lauryl sulfate; Magnesium stearate; Titanium dioxide; Triacetin; Croscarmellose sodium; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses; Polydextrose; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company Lake Eire Medical & Surgical Supply DBA Quality Care Products; Physicians Total Care; RemedyRepack; Stat Rx USA
                   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) [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
Anhydrous lactose; Sodium lauryl sulfate; Magnesium stearate; Titanium dioxide; Triacetin; Croscarmellose sodium; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses; Polydextrose; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company A-S Medication Solutions; Mylan Pharamceuticals; PD-Rx Pharmaceuticals; Raritan Pharmaceuticals; RemedyRepack
                   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) [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 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; Fd&c red no. 40; Magnesium stearate; Titanium dioxide; Aluminum oxide; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Genentech
                   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) [4]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [2]
Magnesium stearate 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
Lactose monohydrate; Magnesium stearate; Titanium dioxide; Polyethylene glycol 400; Hydroxypropyl cellulose (1200000 mw); Hypromellose 2910 (3 mpa.s); Hypromellose 2910 (50 mpa.s); Microcrystalline cellulose
                   Dosage Form Oral Tablet
                   Company A-S Medication Solutions; Bryant Ranch Prepack; Unit Dose Services
                   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) [3]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [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
Lactose monohydrate; Magnesium stearate; Titanium dioxide; Polyethylene glycol 400; Cellulose, microcrystalline; Hydroxypropyl cellulose (type h); Hypromellose 2910 (3 mpa.s); Hypromellose 2910 (50 mpa.s)
                   Dosage Form Oral Tablet
                   Company A-S Medication Solutions; AvKARE; Avera McKennan Hospital; Central Texas Community Health Centers; Denton Pharma; NuCare Pharmaceuticals; RemedyRepack; St Marys Medical Park Pharmacy; 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) [3]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [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
Lactose monohydrate; Magnesium stearate; Titanium dioxide; Hypromellose; Cellulose, microcrystalline; Hydroxypropyl cellulose; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company Keltman Pharmaceuticals
                   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) [6]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
Lactose monohydrate; Magnesium stearate; Titanium dioxide; Polyethylene glycol 400; Cellulose, microcrystalline; Hydroxypropyl cellulose; Hypromelloses
                   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
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [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
Lactose monohydrate; Magnesium stearate; Titanium dioxide; Polyethylene glycol 400; Cellulose, microcrystalline; Hydroxypropyl cellulose (type h); Hypromellose 2910 (3 mpa.s); Hypromellose 2910 (50 mpa.s)
                   Dosage Form Oral Tablet
                   Company RedPharm
                   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) [3]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [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
Lactose monohydrate; Magnesium stearate; Titanium dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose (type h); Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company RemedyRepack
                   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) [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; Magnesium stearate; Titanium dioxide; Hydroxypropyl cellulose (1200000 mw); Hypromellose, unspecified; Microcrystalline cellulose; Polyethylene glycol, unspecified
                   Dosage Form Oral Tablet
                   Company Preferred Pharamaceuticals
                   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) [3]
             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; Magnesium stearate; Titanium dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose (type h); Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Aidarex Pharmaceuticals; Apotheca; Blenheim Phamacal; Cardinal Health; Carilion Materials Management; Clinical Solutions Wholesale; DirectRX; Proficient Rx
                   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) [3]
             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
Lactose monohydrate; Magnesium stearate; Titanium dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose; Hypromelloses; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company H. J. Harkins Company; Rebel Distributors; RemedyRepack
                   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) [3]
             Drug Formulation 13 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; Titanium dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose; Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company RemedyRepack
                   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) [3]
References
1 FDA label for approved ketorolac 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 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
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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