Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00580)
Name
Raltegravir
Synonyms    Click to Show/Hide the Synonyms of This API
Raltegravir; 518048-05-0; MK-0518; Raltegravir (MK-0518); MK0518; UNII-22VKV8053U; N-(2-(4-((4-fluorobenzyl)carbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)propan-2-yl)-5-methyl-1,3,4-oxadiazole-2-carboxamide; 22VKV8053U; MK 0518; 518048-05-0 (free); N-(2-(4-(4-Fluorobenzylcarbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)propan-2-yl)-5-methyl-1,3,4-oxadiazole-2-carboxamide; NCGC00184997-01; DSSTox_CID_28586; DSSTox_RID_82857; DSSTox_GSID_48660; Isentress(TM); 4-Pyrimidinecarboxamide, N-((4-fluorophenyl)methyl)-1,6-dihydro-5-hydroxy-1-methyl-2-(1-methyl-1-(((5-methyl-1,3,4-oxadiazol-2-yl)carbonyl)amino)ethyl)-6-oxo-; N-[2-[4-[(4-fluorophenyl)methylcarbamoyl]-5-hydroxy-1-methyl-6-oxopyrimidin-2-yl]propan-2-yl]-5-methyl-1,3,4-oxadiazole-2-carboxamide; Raltegravir (INN); CAS-518048-05-0; Raltegravir [USAN:INN]; HSDB 8124; N-(4-Fluorobenzyl)-5-Hydroxy-1-Methyl-2-(1-Methyl-1-{[(5-Methyl-1,3,4-Oxadiazol-2-Yl)carbonyl]amino}ethyl)-6-Oxo-1,6-Dihydropyrimidine-4-Carboxamide; N-[1-[4-[(4-fluorophenyl)methylcarbamoyl]-5-hydroxy-1-methyl-6-oxo-pyrimidin-2-yl]-1-methyl-ethyl]-5-methyl-1,3,4-oxadiazole-2-carboxamide; Raltegravir; MK-0518; Raltegravir - MK-0518; Raltegravir(MK-0518)/; hydropyrimidine-4-carboxamide; SCHEMBL51817; cc-110; MLS006011985; SCHEMBL996804; CHEMBL254316; SCHEMBL2112870; DTXSID2048660; BDBM25351; C20H21FN6O5; BCPP000093; HMS3655B09; AOB87131; BCP01394; EX-A2147; Tox21_113019; ABP000913; MFCD10698872; NSC762522; ZINC13831130; AKOS015902444; AKOS025149884; AKOS032960305; Tox21_113019_1; ZINC114994525; AC-5261; CCG-269170; DB06817; MCULE-4916399246; NSC-762522; PB13312; SB20935; NCGC00274066-01; NCGC00274066-05; AK326327; AS-16992; HY-10353; SMR003601806; AB0028054; FT-0649660; SW220138-1; A25486; D06676; MK-0518;MK 0518;MK0518; Q-4458; yl}-6-oxo-1,6-dihydropyrimidine-4-carboxamide; AB01566833_01; 038R721; 048R050; A828788; Q421552; BRD-K05658747-237-01-1; [(5-methyl-1,3,4-oxadiazol-2-yl)formamido]propan-2-; N-[(4-fluorophenyl)methyl]-5-hydroxy-1-methyl-2-{2-; Z1551429745; CN1C(=O)C(=O)\\C(=C(\\O)NCC=2C=CC(F)=CC=2)N=C1C(C)(C)NC(=O)C1=NN=C(C)O1; 4-Pyrimidinecarboxamide, N-((4-fluorophenyl)methyl)-1,6-dihydro-5-hydroxy-1-methyl-2-(1-methyl-1-(((5-methyl-1,3,4-oxadiazol-2-yl)carbonyl)amino)ethyl)-6-oxo- (9CI); MK-0518;N-[(4-Fluorophenyl)methyl]-1,6-dihydro-5-hydroxy-1-methyl-2-[1-methyl-1-[[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino]ethyl]-6-oxo-4-pyrimidinecarboxamide Potassium Salt; N-(2-(4-(4-fluorobenzylcarbamoyl)-5-hydroxy-1-methyl-6-oxo-1, 6-dihydropyrimidin-2-yl)propan-2-yl) -5-methyl-1,3,4-oxadiazole-2- carboxamide; N-(2-(4-(4-Fluorobenzylcarbamoyl)-5-OH-1-Me-6-oxo-pyrimidin-2-yl)propan-2-yl)-5-Me-1,3,4-oxadiazole-2-carboxamide; N-(4-fluorobenzyl)-5-hydroxy-1-methyl-2-(1-methyl-1-{[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino}ethyl)-6-oxo-1,6-di; N-[(4-fluorophenyl)methyl]-5-hydroxy-1-methyl-2-{2-[(5-methyl-1,3,4-oxadiazol-2-yl)formamido]propan-2-yl}-6-oxo-1,6-dihydropyrimidine-4-carboxamide; N-[2-(4-{[(4-fluorophenyl)methyl]carbamoyl}-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)propan-2-yl]-5-methyl-1,3,4-oxadiazole-2-carboxamide; N-[2-[4-[[(4-fluorophenyl)methylamino]-hydroxymethylidene]-1-methyl-5,6-dioxo-2-pyrimidinyl]propan-2-yl]-5-methyl-1,3,4-oxadiazole-2-carboxamide; N-[2-[4-[[(4-fluorophenyl)methylamino]-oxidanyl-methylidene]-1-methyl-5,6-bis(oxidanylidene)pyrimidin-2-yl]propan-2-yl]-5-methyl-1,3,4-oxadiazole-2-carboxamide
Clinical Status
Approved
Disease Indication Human immunodeficiency virus infection ICD-11: 1C60 [1]
PubChem CID
54671008
Formula
C20H21FN6O5
Canonical SMILES
CC1=NN=C(O1)C(=O)NC(C)(C)C2=NC(=C(C(=O)N2C)O)C(=O)NCC3=CC=C(C=C3)F
InChI
1S/C20H21FN6O5/c1-10-25-26-17(32-10)16(30)24-20(2,3)19-23-13(14(28)18(31)27(19)4)15(29)22-9-11-5-7-12(21)8-6-11/h5-8,28H,9H2,1-4H3,(H,22,29)(H,24,30)
InChIKey
CZFFBEXEKNGXKS-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=54671008"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 444.4 Topological Polar Surface Area 150
XlogP 1.1 Complexity 836
Heavy Atom Count 32 Rotatable Bond Count 6
Hydrogen Bond Donor Count 3 Hydrogen Bond Acceptor Count 9
Full List of Drug Formulations (DFMs) Containing This API
          Raltegravir 100 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
Oleic acid; Ammonium glycyrrhizate; Sodium stearyl fumarate; Sucralose; Aspartame; Fructose; Magnesium stearate; Mannitol; Sorbitol; Ammonia; Ferric oxide red; Ferric oxide yellow; Trisodium citrate dihydrate; Medium-chain triglycerides; Polyethylene glycol 400; Crospovidone (15 mpa.s at 5%); Ethylcellulose (20 mpa.s); Hydroxypropyl cellulose (1200000 mw); Hypromellose 2910 (6 mpa.s); Saccharin sodium
                   Dosage Form Chewable Tablet
                   Company Merck Sharp & Dohme
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Monoammonium glycyrrhizate DIG Info Dehydrogenase/reductase 9C 3 (IC50 = 0.4 nM) [2]
Oleic acid DIG Info Liver lipid-binding protein (Ki = 180 nM) [3]
Sucralose DIG Info Carbonic anhydrase II (Ki = 300 nM) [4]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [5]
Aspartame DIG Info Pregnane X receptor (Ki = 13 uM) [6]
Sodium stearyl fumarate DIG Info Leukemia K562 cells (IC50 = 20.2 ug.mL-1) [7]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [8]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [9]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [10]
          Raltegravir 25 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
Oleic acid; Ammonium glycyrrhizate; Sodium stearyl fumarate; Sucralose; Aspartame; Fructose; Magnesium stearate; Mannitol; Sorbitol; Ammonia; Ferric oxide yellow; Trisodium citrate dihydrate; Medium-chain triglycerides; Polyethylene glycol 400; Crospovidone (15 mpa.s at 5%); Ethylcellulose (20 mpa.s); Hydroxypropyl cellulose (1200000 mw); Hypromellose 2910 (6 mpa.s); Saccharin sodium
                   Dosage Form Chewable Tablet
                   Company Merck Sharp & Dohme
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Monoammonium glycyrrhizate DIG Info Dehydrogenase/reductase 9C 3 (IC50 = 0.4 nM) [2]
Oleic acid DIG Info Liver lipid-binding protein (Ki = 180 nM) [3]
Sucralose DIG Info Carbonic anhydrase II (Ki = 300 nM) [4]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [5]
Aspartame DIG Info Pregnane X receptor (Ki = 13 uM) [6]
Sodium stearyl fumarate DIG Info Leukemia K562 cells (IC50 = 20.2 ug.mL-1) [7]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [8]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [9]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [10]
          Raltegravir 400 mg tablet Click to Show/Hide the Full List of Formulation(s):          4 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; Butylated hydroxytoluene; Sodium stearyl fumarate; Magnesium stearate; Anhydrous dibasic calcium phosphate; Ferric oxide red; Ferrosoferric oxide; Talc; Titanium dioxide; Hypromellose; Poloxamer 407; Polyethylene glycol 3350; Polyvinyl alcohol; Cellulose, microcrystalline
                   Dosage Form Oral Tablet
                   Company State of Florida DOH Central Pharmacy
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Butylated hydroxytoluene DIG Info Carbonic anhydrase II (Ki = 630 nM) [11]
Sodium stearyl fumarate DIG Info Leukemia K562 cells (IC50 = 20.2 ug.mL-1) [7]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [12]
Poloxamer 407 DIG Info Albendazole monooxygenase (EC50 = 32.8 uM) [12]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [12]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [8]
Calcium hydrogenphosphate DIG Info Albendazole monooxygenase (Protein expression downregulation) [8]
Polyethylene glycol 3350 DIG Info Albendazole monooxygenase (Protein expression upregulation) [8]
             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; Butylated hydroxytoluene; Sodium stearyl fumarate; Magnesium stearate; Anhydrous dibasic calcium phosphate; Ferric oxide red; Ferrosoferric oxide; Talc; Titanium dioxide; Poloxamer 407; Polyethylene glycol 3350; Polyvinyl alcohol; Cellulose, microcrystalline; Hypromelloses
                   Dosage Form Oral Tablet
                   Company Physicians Total Care
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Butylated hydroxytoluene DIG Info Carbonic anhydrase II (Ki = 630 nM) [11]
Sodium stearyl fumarate DIG Info Leukemia K562 cells (IC50 = 20.2 ug.mL-1) [7]
Poloxamer 407 DIG Info Albendazole monooxygenase (EC50 = 32.8 uM) [12]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [12]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [8]
Calcium hydrogenphosphate DIG Info Albendazole monooxygenase (Protein expression downregulation) [8]
Polyethylene glycol 3350 DIG Info Albendazole monooxygenase (Protein expression upregulation) [8]
             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; Butylated hydroxytoluene; Sodium stearyl fumarate; Magnesium stearate; Anhydrous dibasic calcium phosphate; Ferric oxide red; Ferrosoferric oxide; Talc; Titanium dioxide; Poloxamer 407; Polyethylene glycol 3350; Hypromellose, unspecified; Microcrystalline cellulose; Polyvinyl alcohol, unspecified
                   Dosage Form Oral Tablet
                   Company A-S Medication Solutions; Merck Sharp & Dohme; RemedyRepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Butylated hydroxytoluene DIG Info Carbonic anhydrase II (Ki = 630 nM) [11]
Sodium stearyl fumarate DIG Info Leukemia K562 cells (IC50 = 20.2 ug.mL-1) [7]
Poloxamer 407 DIG Info Albendazole monooxygenase (EC50 = 32.8 uM) [12]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [8]
Calcium hydrogenphosphate DIG Info Albendazole monooxygenase (Protein expression downregulation) [8]
Polyethylene glycol 3350 DIG Info Albendazole monooxygenase (Protein expression upregulation) [8]
             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; Butylated hydroxytoluene; Sodium stearyl fumarate; Magnesium stearate; Ferric oxide red; Ferrosoferric oxide; Talc; Titanium dioxide; Poloxamer 407; Polyethylene glycol 3350; Polyvinyl alcohol; Calcium phosphate, dibasic, anhydrous; Cellulose, microcrystalline; Hypromelloses
                   Dosage Form Oral Tablet
                   Company A-S Medication Solutions; Avera McKennan Hospital; Dispensing Solution; NuCare Pharmaceuticals; RemedyRepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Butylated hydroxytoluene DIG Info Carbonic anhydrase II (Ki = 630 nM) [11]
Sodium stearyl fumarate DIG Info Leukemia K562 cells (IC50 = 20.2 ug.mL-1) [7]
Poloxamer 407 DIG Info Albendazole monooxygenase (EC50 = 32.8 uM) [12]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [12]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [8]
Polyethylene glycol 3350 DIG Info Albendazole monooxygenase (Protein expression upregulation) [8]
          Raltegravir Potassium eq 100mg base/packet powder 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
Ammonium Hydroxide; Banana With Other Natural Flavors; Carboxymethylcellulose Sodium; Crospovidone; Ethylcellulose 20 Cp; Fructose; Hydroxypropyl Cellulose; Hypromellose 2910/6Cp; Macrogol/Peg 400; Magnesium Stearate; Maltodextrin; Mannitol; Medium Chain Triglycerides; Microcrystalline Cellulose; Monoammonium Glycyrrhizinate; Oleic Acid; Sorbitol; Sucralose; Sucrose
                   Dosage Form Powder
                   Company Merck Sharp Dohme
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Monoammonium glycyrrhizate DIG Info Dehydrogenase/reductase 9C 3 (IC50 = 0.4 nM) [2]
Oleic acid DIG Info Liver lipid-binding protein (Ki = 180 nM) [3]
Sucralose DIG Info Carbonic anhydrase II (Ki = 300 nM) [4]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [5]
Carboxymethylcellulose sodium DIG Info Albendazole monooxygenase (EC50 = 12.6 uM) [12]
Hydroxypropyl cellulose DIG Info Mephenytoin 4-hydroxylase (EC50 = 89.5 uM) [12]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [12]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [8]
Dextrin DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 55 %) [9]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [8]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [9]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [10]
          Raltegravir Potassium eq 25mg base Chewable 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
Ammonium Hydroxide; Crospovidone; Ethylcellulose 20 Cp; Fructose; Hydroxypropyl Cellulose; Hypromellose 2910/6Cp; Magnesium Stearate; Mannitol; Medium Chain Triglycerides; Monoammonium Glycyrrhizinate; Natural And Artificial Flavors (Orange, Banana, And Masking That Contains Aspartame); Oleic Acid; Peg 400; Saccharin Sodium; Sodium Citrate Dihydrate; Sodium Stearyl Fumarate; Sorbitol; Sucralose And Yellow Iron Oxide; Red Iron Oxide
                   Dosage Form Chewable Tablet
                   Company Merck Sharp Dohme
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Monoammonium glycyrrhizate DIG Info Dehydrogenase/reductase 9C 3 (IC50 = 0.4 nM) [2]
Oleic acid DIG Info Liver lipid-binding protein (Ki = 180 nM) [3]
Sucralose DIG Info Carbonic anhydrase II (Ki = 300 nM) [4]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [5]
Saccharin sodium anhydrous DIG Info Carbonic anhydrase I (Ki = 18540 nM) [13]
Sodium stearyl fumarate DIG Info Leukemia K562 cells (IC50 = 20.2 ug.mL-1) [7]
Hydroxypropyl cellulose DIG Info Mephenytoin 4-hydroxylase (EC50 = 89.5 uM) [12]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [12]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [8]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [8]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [9]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [10]
          Raltegravir Potassium eq 100mg base Chewable 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
Ammonium Hydroxide; Crospovidone; Ethylcellulose 20 Cp; Fructose; Hydroxypropyl Cellulose; Hypromellose 2910/6Cp; Magnesium Stearate; Mannitol; Medium Chain Triglycerides; Monoammonium Glycyrrhizinate; Natural And Artificial Flavors (Orange, Banana, And Masking That Contains Aspartame); Oleic Acid; Peg 400; Saccharin Sodium; Sodium Citrate Dihydrate; Sodium Stearyl Fumarate; Sorbitol; Sucralose And Yellow Iron Oxide; Red Iron Oxide
                   Dosage Form Chewable Tablet
                   Company Merck Sharp Dohme
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Monoammonium glycyrrhizate DIG Info Dehydrogenase/reductase 9C 3 (IC50 = 0.4 nM) [2]
Oleic acid DIG Info Liver lipid-binding protein (Ki = 180 nM) [3]
Sucralose DIG Info Carbonic anhydrase II (Ki = 300 nM) [4]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [5]
Saccharin sodium anhydrous DIG Info Carbonic anhydrase I (Ki = 18540 nM) [13]
Sodium stearyl fumarate DIG Info Leukemia K562 cells (IC50 = 20.2 ug.mL-1) [7]
Hydroxypropyl cellulose DIG Info Mephenytoin 4-hydroxylase (EC50 = 89.5 uM) [12]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [12]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [8]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [8]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [9]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [10]
          Raltegravir Potassium eq 400mg base 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
Calcium Phosphate Dibasic Anhydrous; Hypromellose 2208; Lactose Monohydrate; Magnesium Stearate; Microcrystalline Cellulose; Poloxamer 407 (Contains 0.01% Butylated Hydroxytoluene As Antioxidant); Sodium Stearyl Fumarate; Black Iron Oxide; Polyethylene Glycol 3350; Polyvinyl Alcohol; Red Iron Oxide; Talc; Titanium Dioxide
                   Dosage Form Tablet
                   Company Merck Sharp Dohme
                   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]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [12]
Poloxamer 407 DIG Info Albendazole monooxygenase (EC50 = 32.8 uM) [12]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [12]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [8]
Calcium hydrogenphosphate DIG Info Albendazole monooxygenase (Protein expression downregulation) [8]
Polyethylene glycol 3350 DIG Info Albendazole monooxygenase (Protein expression upregulation) [8]
          Raltegravir Potassium eq 600mg base 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
Croscarmellose Sodium; Hypromellose 2910; Magnesium Stearate; Microcrystalline Cellulose; Ferrosoferric Oxide; Hypromellose 2910; Iron Oxide Yellow; Lactose Monohydrate; Triacetin; Titanium Dioxide; Carnauba Wax
                   Dosage Form Tablet
                   Company Merck Sharp Dohme
                   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) [12]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [8]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [8]
          Raltegravir 600 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
Lactose monohydrate; Magnesium stearate; Ferric oxide yellow; Ferrosoferric oxide; Titanium dioxide; Triacetin; Croscarmellose sodium; Carnauba wax; Hypromellose, unspecified; Microcrystalline cellulose
                   Dosage Form Oral Tablet
                   Company Merck Sharp & Dohme
                   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) [8]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [8]
References
1 2007 FDA drug approvals: a year of flux. Nat Rev Drug Discov. 2008 Feb;7(2):107-9.
2 Cycloartane and friedelane triterpenoids from the leaves of Caloncoba glauca and their evaluation for inhibition of 11-hydroxysteroid dehydrogenases. J Nat Prod. 2012 Apr 27; 75(4):599-604.
3 Characterization of the drug binding specificity of rat liver fatty acid binding protein. J Med Chem. 2008 Jul 10; 51(13):3755-64.
4 Sweet Binders: Carbonic Anhydrase IX in Complex with Sucralose. ACS Med Chem Lett. 2018 May 10; 9(7):657-661.
5 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.
6 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
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 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
9 Interactions between human multidrug resistance related protein (MRP2; ABCC2) and excipients commonly used in self-emulsifying drug delivery systems (SEDDS). Int J Pharm. 2013 Apr 15;447(1-2):192-8.
10 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
11 Carbonic anhydrase inhibitors. Inhibition of human erythrocyte isozymes I and II with a series of antioxidant phenols. Bioorg Med Chem. 2009 Apr 15; 17(8):3207-11.
12 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
13 Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides. Bioorg Med Chem. 2009 Jul 15; 17(14):5054-8.

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