Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00517)
Name
Pentoxifylline
Synonyms    Click to Show/Hide the Synonyms of This API
pentoxifylline; Trental; Oxpentifylline; Pentoxifyllin; Torental; Pentoxyphylline; Dimethyloxohexylxanthine; Pentoxiphyllium; Vazofirin; Pentoxiphylline; Rentylin; 3,7-Dimethyl-1-(5-oxohexyl)xanthine; BL 191; Pentoxyphyllin; 3,7-Dihydro-3,7-dimethyl-1-(5-oxohexyl)-1H-purine-2,6-dione; 1-(5-Oxohexyl)theobromine; 3,7-dimethyl-1-(5-oxohexyl)purine-2,6-dione; 3,7-Dimethyl-1-(5-oxohexyl)-3,7-dihydro-1H-purine-2,6-dione; BL-191; 1H-Purine-2,6-dione, 3,7-dihydro-3,7-dimethyl-1-(5-oxohexyl)-; Pentoxyfilline; 1-(5-Oxohexyl)-3,7-dimethylxanthine; Theobromine, 1-(5-oxohexyl)-; SD6QCT3TSU; UNII-SD6QCT3TSU; 3,7-dimethyl-1-(5-oxohexyl)-1H-purine-2,6(3H,7H)-dione; MFCD00063379; NSC637086; CHEMBL628; NSC 637086; 1,2,3,6-Tetrahydro-3,7-dimethyl-1-(5-oxohexyl)-2,6-purindion; 3,7-Dimethyl-1-(5-oxohexyl)-1H,3H-purin-2,6-dione; MLS000079026; CHEBI:7986; Pentoxyfylline; Azupentat; EHT 0202; NSC-637086; NCGC00015801-02; Durapental; SMR000035998; 3,7-dimethyl-1-(5-oxohexyl)-2,3,6,7-tetrahydro-1H-purine-2,6-dione; DSSTox_CID_3437; DSSTox_RID_77028; DSSTox_GSID_23437; Pentoxifyllinum; Pentoxifilina; Pentoxiphyllin; Hemovas; Ralofect; Vasofirin; Ikomio; Agapurin Retard; Pentoxifilina [INN-Spanish]; Pentoxifyllinum [INN-Latin]; Pentoxil (TN); Trental (TN); CAS-6493-05-6; EHT0201; SR-01000075641; 3,7-Dimethyl-1-(5-oxohexyl)xantine; 3,7-Dimethyl-1-(5-oxohexyl) xantine; Pentoxyifylline; Pentopak; CCRIS 6832; Pentoxifylline (JAN/USP/INN); C04AD03; EHT-201; PTX;Oxpentifylline; EHT-0201; Prestwick_608; EINECS 229-374-5; Pentoxifylline,(S); BRN 0558929; Spectrum_001444; Opera_ID_1800; Prestwick0_000196; Prestwick1_000196; Prestwick2_000196; Prestwick3_000196; Spectrum2_001181; Spectrum3_001820; Spectrum4_000227; Spectrum5_001161; Lopac-P-1784; P 1784; Lopac0_000936; SCHEMBL34039; BSPBio_000151; BSPBio_003439; KBioGR_000893; KBioSS_001924; MLS000758298; MLS001201764; MLS001424051; BIDD:GT0174; DivK1c_000729; SPECTRUM1503611; SPBio_001221; SPBio_002072; BPBio1_000167; GTPL7095; DTXSID7023437; BDBM10850; HMS502E11; KBio1_000729; KBio2_001924; KBio2_004492; KBio2_007060; KBio3_002942; NINDS_000729; HMS1568H13; HMS1922E16; HMS2051N06; HMS2090H13; HMS2093G21; HMS2095H13; HMS2235C16; HMS3262L14; HMS3370D09; HMS3393N06; HMS3712H13; Pharmakon1600-01503611; BCP29306; HY-B0715; ZINC1530776; Tox21_110223; Tox21_500936; BBL016497; CCG-36382; NSC758481; PDSP1_001015; PDSP2_000999; STK177321; AKOS000541484; Tox21_110223_1; AC-8381; DB00806; LP00936; MCULE-9951939936; NC00255; NSC-758481; SDCCGSBI-0050910.P004; VZ33607; 3,7-dimethyl-1-(5-oxohexyl)-xanthine; CAS-1677687; IDI1_000729; NCGC00015801-01; NCGC00015801-03; NCGC00015801-04; NCGC00015801-05; NCGC00015801-06; NCGC00015801-07; NCGC00015801-08; NCGC00015801-09; NCGC00015801-10; NCGC00015801-12; NCGC00015801-17; NCGC00015801-21; NCGC00067069-02; NCGC00067069-03; NCGC00067069-04; NCGC00067069-05; NCGC00178062-01; NCGC00178062-02; NCGC00261621-01; AS-13662; Pentoxifylline [USAN:USP:INN:BAN:JAN]; SBI-0050910.P003; 1-(5-oxohexyl)theobromine (pentoxifylline); AB00052363; EU-0100936; FT-0603570; FT-0657886; FT-0673610; ST50242554; SW196777-4; C07424; D00501; J10071; AB00052363-17; AB00052363_18; AB00052363_21; 5-26-14-00081 (Beilstein Handbook Reference); Q416331; 3,7-dimethyl-1-(5-oxohexyl)-1H-purine-2,6-dione; PTX; Oxpentifylline; BL191; BL 191; BL-191; SR-01000075641-1; SR-01000075641-4; SR-01000075641-7; SR-01000075641-9; BRD-K57569181-001-05-1; BRD-K57569181-001-16-8; 3,7-dimethyl-1-(5-oxohexyl)-3,7-dihydropurine-2,6-dione; 3,7-dimethyl-1-(5-oxohexyl)-1,3,7-trihydropurine-2,6-dione; 3,7-Dimethyl-1-(5-oxohexyl)-3,7-dihydro-1H-purine-2,6-dione #
Clinical Status
Approved
Disease Indication Intermittent claudication ICD-11: BD40 [1]
PubChem CID
4740
Formula
C13H18N4O3
Canonical SMILES
CC(=O)CCCCN1C(=O)C2=C(N=CN2C)N(C1=O)C
InChI
1S/C13H18N4O3/c1-9(18)6-4-5-7-17-12(19)10-11(14-8-15(10)2)16(3)13(17)20/h8H,4-7H2,1-3H3
InChIKey
BYPFEZZEUUWMEJ-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=4740"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 278.31 Topological Polar Surface Area 75.5
XlogP 0.3 Complexity 426
Heavy Atom Count 20 Rotatable Bond Count 5
Hydrogen Bond Donor Count 0 Hydrogen Bond Acceptor Count 4
Full List of Drug Formulations (DFMs) Containing This API
          Pentoxifylline 400 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
D&c red no. 30; Fd&c blue no. 2; Fd&c yellow no. 6; Magnesium stearate; Titanium dioxide; Triacetin; Hypromellose; Povidone; Cellulose, microcrystalline; Hydroxyethyl cellulose (140 cps at 5%); Polydextrose; Polyethylene glycol
                   Dosage Form Extended Release 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
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
D&C red no. 30 DIG Info Heat shock factor 1 (EC50 = 9054 nM) [4]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [5]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
D&c red no. 30; Fd&c blue no. 2; Fd&c yellow no. 6; Magnesium stearate; Titanium dioxide; Triacetin; Povidone; Cellulose, microcrystalline; Hydroxyethyl cellulose (140 cps at 5%); Hypromelloses; Polydextrose; Polyethylene glycol
                   Dosage Form Extended Release Oral Tablet
                   Company Cardinal Health
                   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]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
D&C red no. 30 DIG Info Heat shock factor 1 (EC50 = 9054 nM) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
D&c red no. 30; Fd&c blue no. 2; Fd&c yellow no. 6; Magnesium stearate; Titanium dioxide; Triacetin; Povidone; Cellulose, microcrystalline; Hydroxyethyl cellulose (140 mpa.s at 5%); Hypromelloses; Polydextrose; Polyethylene glycols
                   Dosage Form Extended Release Oral Tablet
                   Company McKesson
                   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]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
D&C red no. 30 DIG Info Heat shock factor 1 (EC50 = 9054 nM) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
D&c red no. 30; Fd&c blue no. 2; Fd&c yellow no. 6; Magnesium stearate; Titanium dioxide; Triacetin; Cellulose, microcrystalline; Hydroxyethyl cellulose (140 cps at 5%); Hypromelloses; Polydextrose; Polyethylene glycols; Povidones
                   Dosage Form Extended Release Oral Tablet
                   Company RemedyRepack
                   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]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
D&C red no. 30 DIG Info Heat shock factor 1 (EC50 = 9054 nM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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
D&c red no. 30; Fd&c blue no. 2; Fd&c yellow no. 6; Magnesium stearate; Titanium dioxide; Triacetin; Cellulose, microcrystalline; Hydroxyethyl cellulose (140 mpa.s at 5%); Hypromelloses; Polydextrose; Polyethylene glycols; Povidones
                   Dosage Form Extended Release Oral Tablet
                   Company Mylan Pharamceuticals; NCS HealthCare of KY, Inc dba Vangard Labs
                   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]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
D&C red no. 30 DIG Info Heat shock factor 1 (EC50 = 9054 nM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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
Isopropyl alcohol; Magnesium stearate; Talc; Povidone; Hydroxyethyl cellulose (2000 cps at 1%)
                   Dosage Form Extended Release Oral Tablet
                   Company PD-Rx Pharmaceuticals; Stat Rx USA
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [7]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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
Isopropyl alcohol; Magnesium stearate; Talc; Povidone
                   Dosage Form Extended Release 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
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [7]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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
Isopropyl alcohol; Magnesium stearate; Talc; Hydroxyethyl cellulose (2000 mpa.s at 1%)
                   Dosage Form Extended Release Oral Tablet
                   Company A-S Medication Solutions; AvKARE; Lake Eire Medical & Surgical Supply DBA Quality Care Products; Physicians Total Care; Teva Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [7]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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
Isopropyl alcohol; Magnesium stearate; Talc; Povidones
                   Dosage Form Extended Release Oral Tablet
                   Company Aphena Pharma Solutions-Tennessee; Oceanside Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [7]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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; Talc; Titanium dioxide; Fd&c red no. 3; Povidone; Hypromelloses; Polyethylene glycols
                   Dosage Form Extended Release Tablet
                   Company Sanofi-Aventis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C red no. 3 DIG Info Phosphodiesterase 3A (IC50 = 0.092 uM) [3]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [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; Silicon dioxide; Hydroxypropyl cellulose (1200000 mw); Hypromellose, unspecified; Polyethylene glycol 8000
                   Dosage Form Extended Release 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) [6]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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; Titanium dioxide; Silicon dioxide; Hydroxypropyl cellulose; Hypromelloses; Polyethylene glycol 8000
                   Dosage Form Extended Release Oral Tablet
                   Company Aphena Pharma Solutions-Tennessee; Bryant Ranch Prepack; Golden State Medical Supply
                   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) [6]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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
Magnesium stearate; Titanium dioxide; Silicon dioxide; Hydroxypropyl cellulose (type h); Hypromelloses; Polyethylene glycol 8000
                   Dosage Form Extended Release Oral Tablet
                   Company Aidarex Pharmaceuticals; NuCare 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) [6]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
References
1 FDA label for approved pentoxifylline 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 PubChem BioAssay data set.
5 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
6 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
7 Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. J Med Chem. 2004 Mar 11; 47(6):1413-22.

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