Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00159)
Name
Cyclosporin A
Synonyms    Click to Show/Hide the Synonyms of This API
cyclosporin A; cyclosporine; Ciclosporin; 59865-13-3; Cyclosporine A; Sandimmune; Sandimmun; Neoral; Cyclosporin; Ciclosporine; Gengraf; Ramihyphin A; Sandimmun Neoral; Sang-35; Ciclosporina; Ciclosporinum; Consupren; Equoral; Neoplanta; UNII-83HN0GTJ6D; Antibiotic S 7481F1; SangCyA; MFCD00274558; 83HN0GTJ6D; MLS001333756; CHEBI:4031; S-Neoral; Cipol N; Sigmasporin Microoral; Cyclosporin A solution; DSSTox_CID_365; Ciclosporin (Ciclosporin A); DSSTox_RID_75541; DSSTox_GSID_20365; SDZ-OXL 400; Ciclosporin A; OL 27-400; Abrammune; Imusporin; Optimmune; Seciera; Vekacia; Papilock Mini; Arpimune ME; Zinograf ME; Sandimmune Neoral; Ciclosporina Germed; SMR000058578; Cicloral (antibiotic); Debio088; Sang 35; Cyclosporine [USAN:USP]; Ciclosporine [INN-French]; Ciclosporinum [INN-Latin]; Ciclosporina [INN-Spanish]; Cyclospori; Sigmasporin; Cyclokat; Mitogard; Papilock; Pulminiq; Zyclorin; CicloMulsion; Ciclosporin;; CCRIS 1590; Ciclosporin DT; Consupren S; NSC290193; Modusik-A; HSDB 6881; NeuroSTAT; NSC-290193; Cipol-N; NCGC00016890-01; DRG-0275; Prestwick_731; Ciclosporin [INN]; CAS-59865-13-3; NSC 290193; CsA & IFN.alpha.; S 7481F1; Cyclosporine manufacturer; Prestwick2_000435; Prestwick3_000435; CHEMBL160; Sang-2000; SCHEMBL3491; SCHEMBL4442; Nova-22007; Ikervis (opthalmic solution); BSPBio_000450; Cyclosporin A & IFN.alpha.; MLS000028376; MLS002153454; MLS002207033; Verkazia (opthalmic solution); SDZ-OXL-400; BPBio1_000496; GTPL1024; ANTIBIOTIC S-7481F1; DTXSID0020365; CHEBI:92233; AOB2581; ATH-002; OLO-400; CB-01-09 MMX; HMS1569G12; HMS2089A09; HMS2096G12; HMS2230M14; HMS3713G12; Cyclosporin A, Ready Made Solution; EX-A4110; HY-B0579; Tox21_110667; Tox21_301849; BDBM50022815; DE-076; ST-603; Cyclosporin A, >=98.5% (TLC); AKOS015969287; Tox21_110667_1; CCG-208184; DB00091; EBD2126862; KS-1257; SDCCGSBI-0050230.P004; NCGC00093704-12; NCGC00164258-01; NCGC00164258-02; NCGC00164258-03; NCGC00255232-01; AT-12519; OL-27400; SBI-0050230.P003; AB0090560; OL-27-400; 5946-EP0930075A1; 5946-EP2289877A1; 5946-EP2292601A1; 5946-EP2292602A1; 5946-EP2292603A1; 5946-EP2292604A2; 5946-EP2292618A1; 5946-EP2293650A1; 5946-EP2298737A1; 5946-EP2298739A1; 5946-EP2298740A1; 5946-EP2298741A1; 5946-EP2298771A2; 5946-EP2301920A1; 5946-EP2301940A1; 5946-EP2308843A1; 5946-EP2308861A1; J10181; J90049; 865C133; Cyclosporin A, VETRANAL(TM), analytical standard; Q367700; SR-01000780563; Q-200913; SR-01000780563-3; BRD-K03222093-001-01-8; BRD-K13533483-001-03-0; Ciclosporin, European Pharmacopoeia (EP) Reference Standard; Cyclosporin A, from Tolypocladium inflatum, >=95% (HPLC), solid; Cyclosporine, United States Pharmacopeia (USP) Reference Standard; Cyclosporine, Pharmaceutical Secondary Standard; Certified Reference Material; 104250-72-8
Clinical Status
Approved
Disease Indication Rheumatoid arthritis ICD-11: FA20 [1]
PubChem CID
5284373
Formula
C62H111N11O12
Canonical SMILES
CC[C@H]1C(=O)N(CC(=O)N([C@H](C(=O)N[C@H](C(=O)N([C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N([C@H](C(=O)N([C@H](C(=O)N([C@H](C(=O)N([C@H](C(=O)N1)[C@@H]([C@H](C)C/C=C/C)O)C)C(C)C)C)CC(C)C)C)CC(C)C)C)C)C)CC(C)C)C)C(C)C)CC(C)C)C)C
InChI
1S/C62H111N11O12/c1-25-27-28-40(15)52(75)51-56(79)65-43(26-2)58(81)67(18)33-48(74)68(19)44(29-34(3)4)55(78)66-49(38(11)12)61(84)69(20)45(30-35(5)6)54(77)63-41(16)53(76)64-42(17)57(80)70(21)46(31-36(7)8)59(82)71(22)47(32-37(9)10)60(83)72(23)50(39(13)14)62(85)73(51)24/h25,27,34-47,49-52,75H,26,28-33H2,1-24H3,(H,63,77)(H,64,76)(H,65,79)(H,66,78)/b27-25+/t40-,41+,42-,43+,44+,45+,46+,47+,49+,50+,51+,52-/m1/s1
InChIKey
PMATZTZNYRCHOR-CGLBZJNRSA-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=5284373"></iframe>
3D MOL is unavailable 2D MOL
Physicochemical Properties Molecular Weight 1202.6 Topological Polar Surface Area 279
XlogP 7.5 Complexity 2330
Heavy Atom Count 85 Rotatable Bond Count 15
Hydrogen Bond Donor Count 5 Hydrogen Bond Acceptor Count 12
Full List of Drug Formulations (DFMs) Containing This API
          Cyclosporin A 100 mg capsule 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
Sodium lauryl sulfate; D&c yellow no. 10; Fd&c red no. 40; Butyl alcohol; Fd&c blue no. 1; Fd&c blue no. 2; Ferric oxide red; Ferrosoferric oxide; Propylene glycol; Talc; Titanium dioxide; Water; Alcohol; Gelatin; Methyl alcohol; Shellac
                   Dosage Form Oral Capsule
                   Company Apotex; Physicians Total Care
                   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) [2]
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [2]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [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
Sodium lauryl sulfate; D&c yellow no. 10; Fd&c red no. 40; Butyl alcohol; Fd&c blue no. 1; Fd&c blue no. 2; Ferric oxide red; Ferrosoferric oxide; Propylene glycol; Talc; Titanium dioxide; Water; Alcohol; Gelatin, unspecified; Methyl alcohol; Shellac
                   Dosage Form Oral Capsule
                   Company American Health Packaging
                   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) [2]
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [2]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [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
Glycine; Alpha.-tocopherol, dl-; Fd&c blue no. 2; Sorbitol; Glycerin; Propylene glycol; Titanium dioxide; Polyoxyl 40 hydrogenated castor oil; Alcohol; Aluminum oxide; Brown iron oxide; Gelatin; Polyglyceryl-10 oleate; Polyglyceryl-3 oleate; Shellac
                   Dosage Form Oral Capsule
                   Company IVAX Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Aminoethanoic acid DIG Info Glycine type-1 transporter (IC50 = 31600 nM) [5]
DL-alpha-tocopherol DIG Info Presenilin 1 (EC50 > 100000 nM) [6]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Hydrogenated polyoxyl 40 castor oil DIG Info Cytochrome P450 2C9 (IC50 = 30 uM) [7]
             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
Glycine; Alpha.-tocopherol, dl-; Fd&c blue no. 2; Sorbitol; Titanium dioxide; Polyoxyl 40 hydrogenated castor oil; Aluminum oxide; Gelatin
                   Dosage Form Oral Capsule
                   Company Cardinal Health; Physicians Total Care
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Aminoethanoic acid DIG Info Glycine type-1 transporter (IC50 = 31600 nM) [5]
DL-alpha-tocopherol DIG Info Presenilin 1 (EC50 > 100000 nM) [6]
Hydrogenated polyoxyl 40 castor oil DIG Info Cytochrome P450 2C9 (IC50 = 30 uM) [7]
             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
Sorbitan monooleate; Fd&c blue no. 2; Propylene glycol; Titanium dioxide; Polyoxyl 35 castor oil; Polysorbate 80; Alcohol; Gelatin; Polyethylene glycols
                   Dosage Form Oral Capsule
                   Company AbbVie
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Polyoxyl 35 castor oil DIG Info Cholesterol 25-hydroxylase (EC50 = 1.1 uM) [8]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
             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
Sorbitan monooleate; Fd&c blue no. 2; Propylene glycol; Titanium dioxide; Polyoxyl 35 castor oil; Polysorbate 80; Alcohol; Gelatin, unspecified; Polyethylene glycol, unspecified
                   Dosage Form Oral Capsule
                   Company Cardinal Health
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Polyoxyl 35 castor oil DIG Info Cholesterol 25-hydroxylase (EC50 = 1.1 uM) [8]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
             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
Alpha-tocopherol; Sorbitol; Glyceryl monocaprylate; Ferric oxide red; Glycerin; Titanium dioxide; Medium-chain triglycerides; Polyoxyl 35 castor oil; Gelatin; Peg-8 caprylic/capric glycerides; Shellac
                   Dosage Form Oral Capsule
                   Company Actavis Pharma
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Alpha-tocopherol DIG Info Glutathione S-transferase P (IC50 = 500 nM) [9]
Polyoxyl 35 castor oil DIG Info Cholesterol 25-hydroxylase (EC50 = 1.1 uM) [8]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [10]
             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
Alpha.-tocopherol; Sorbitol; Glyceryl monocaprylate; Ferric oxide red; Glycerin; Titanium dioxide; Medium-chain triglycerides; Polyoxyl 35 castor oil; Gelatin, unspecified; Peg-8 caprylic/capric glycerides; Shellac
                   Dosage Form Oral Capsule
                   Company Mayne Pharma
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Alpha-tocopherol DIG Info Glutathione S-transferase P (IC50 = 500 nM) [9]
Polyoxyl 35 castor oil DIG Info Cholesterol 25-hydroxylase (EC50 = 1.1 uM) [8]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [10]
             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
Cochineal; Ferrosoferric oxide; Glycerin; Propylene glycol; Titanium dioxide; Polyoxyl 40 hydrogenated castor oil; Corn oil; Gelatin; Tocopherol
                   Dosage Form Oral Capsule
                   Company Novartis Pharmaceuticals Corporation
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Caprylic acid DIG Info GPCR84 receptor (Ki = 19600 nM) [11]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Hydrogenated polyoxyl 40 castor oil DIG Info Cytochrome P450 2C9 (IC50 = 30 uM) [7]
             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
Glycine; Alpha.-tocopherol, dl-; Sorbitol; Glycerin; Titanium dioxide; Polyoxyl 40 hydrogenated castor oil; Alcohol; Brown iron oxide; Gelatin; Polyglyceryl-10 oleate; Polyglyceryl-3 oleate
                   Dosage Form Oral Capsule
                   Company Teva Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Aminoethanoic acid DIG Info Glycine type-1 transporter (IC50 = 31600 nM) [5]
DL-alpha-tocopherol DIG Info Presenilin 1 (EC50 > 100000 nM) [6]
Hydrogenated polyoxyl 40 castor oil DIG Info Cytochrome P450 2C9 (IC50 = 30 uM) [7]
             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
Alpha.-tocopherol, dl-; Polyoxyl 35 castor oil; Alcohol; Corn oil; Polyethylene glycols
                   Dosage Form Oral Capsule
                   Company Elanco US
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
DL-alpha-tocopherol DIG Info Presenilin 1 (EC50 > 100000 nM) [6]
Polyoxyl 35 castor oil DIG Info Cholesterol 25-hydroxylase (EC50 = 1.1 uM) [8]
             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
Sorbitol; Glycerin; Polyethylene glycol 400; Polyoxyl 40 hydrogenated castor oil; Tocophersolan; Alcohol; Gelatin
                   Dosage Form Oral Capsule
                   Company Eon Labs
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Hydrogenated polyoxyl 40 castor oil DIG Info Cytochrome P450 2C9 (IC50 = 30 uM) [7]
Tocophersolan DIG Info Albendazole monooxygenase (EC50 = 28.3 uM) [8]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [4]
             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
Sorbitol; Ferric oxide red; Glycerin; Titanium dioxide; Alcohol; Castor oil; Corn oil; Gelatin; Olive oil
                   Dosage Form Oral Capsule
                   Company Novartis Pharmaceuticals Corporation
          Cyclosporin A 25 mg capsule Click to Show/Hide the Full List of Formulation(s):        11 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
Sodium lauryl sulfate; D&c yellow no. 10; Fd&c red no. 40; Butyl alcohol; Fd&c blue no. 1; Fd&c blue no. 2; Ferric oxide red; Ferrosoferric oxide; Propylene glycol; Talc; Titanium dioxide; Water; Alcohol; Gelatin; Methyl alcohol; Shellac
                   Dosage Form Oral Capsule
                   Company Apotex
                   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) [2]
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [2]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [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
Sodium lauryl sulfate; D&c yellow no. 10; Fd&c red no. 40; Butyl alcohol; Fd&c blue no. 1; Fd&c blue no. 2; Ferric oxide red; Ferrosoferric oxide; Propylene glycol; Talc; Titanium dioxide; Water; Alcohol; Gelatin, unspecified; Methyl alcohol; Shellac
                   Dosage Form Oral Capsule
                   Company American Health Packaging
                   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) [2]
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [2]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [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
Glycine; Alpha.-tocopherol, dl-; Fd&c blue no. 2; Sorbitol; Ferric oxide yellow; Glycerin; Propylene glycol; Titanium dioxide; Polyoxyl 40 hydrogenated castor oil; Alcohol; Aluminum oxide; Gelatin; Polyglyceryl-10 oleate; Polyglyceryl-3 oleate; Shellac
                   Dosage Form Oral Capsule
                   Company IVAX Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Aminoethanoic acid DIG Info Glycine type-1 transporter (IC50 = 31600 nM) [5]
DL-alpha-tocopherol DIG Info Presenilin 1 (EC50 > 100000 nM) [6]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Hydrogenated polyoxyl 40 castor oil DIG Info Cytochrome P450 2C9 (IC50 = 30 uM) [7]
             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
Sorbitan monooleate; Fd&c blue no. 2; Propylene glycol; Titanium dioxide; Polyoxyl 35 castor oil; Polysorbate 80; Alcohol; Gelatin; Polyethylene glycols
                   Dosage Form Oral Capsule
                   Company AbbVie
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Polyoxyl 35 castor oil DIG Info Cholesterol 25-hydroxylase (EC50 = 1.1 uM) [8]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
             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
Alpha-tocopherol; Sorbitol; Glyceryl monocaprylate; Ferric oxide red; Glycerin; Titanium dioxide; Medium-chain triglycerides; Polyoxyl 35 castor oil; Gelatin; Peg-8 caprylic/capric glycerides; Shellac
                   Dosage Form Oral Capsule
                   Company Actavis Pharma
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Alpha-tocopherol DIG Info Glutathione S-transferase P (IC50 = 500 nM) [9]
Polyoxyl 35 castor oil DIG Info Cholesterol 25-hydroxylase (EC50 = 1.1 uM) [8]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [10]
             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
Alpha.-tocopherol; Sorbitol; Glyceryl monocaprylate; Ferric oxide red; Glycerin; Titanium dioxide; Medium-chain triglycerides; Polyoxyl 35 castor oil; Gelatin, unspecified; Peg-8 caprylic/capric glycerides; Shellac
                   Dosage Form Oral Capsule
                   Company Mayne Pharma
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Alpha-tocopherol DIG Info Glutathione S-transferase P (IC50 = 500 nM) [9]
Polyoxyl 35 castor oil DIG Info Cholesterol 25-hydroxylase (EC50 = 1.1 uM) [8]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [10]
             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
Glycine; Alpha.-tocopherol, dl-; Sorbitol; Ferric oxide yellow; Glycerin; Titanium dioxide; Polyoxyl 40 hydrogenated castor oil; Alcohol; Gelatin; Polyglyceryl-10 oleate; Polyglyceryl-3 oleate
                   Dosage Form Oral Capsule
                   Company Teva Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Aminoethanoic acid DIG Info Glycine type-1 transporter (IC50 = 31600 nM) [5]
DL-alpha-tocopherol DIG Info Presenilin 1 (EC50 > 100000 nM) [6]
Hydrogenated polyoxyl 40 castor oil DIG Info Cytochrome P450 2C9 (IC50 = 30 uM) [7]
             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
Cochineal; Ferrosoferric oxide; Glycerin; Propylene glycol; Titanium dioxide; Polyoxyl 40 hydrogenated castor oil; Corn oil; Gelatin; Tocopherol
                   Dosage Form Oral Capsule
                   Company Cardinal Health; Novartis Pharmaceuticals Corporation
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Caprylic acid DIG Info GPCR84 receptor (Ki = 19600 nM) [11]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Hydrogenated polyoxyl 40 castor oil DIG Info Cytochrome P450 2C9 (IC50 = 30 uM) [7]
             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
Alpha.-tocopherol, dl-; Polyoxyl 35 castor oil; Alcohol; Corn oil; Polyethylene glycols
                   Dosage Form Oral Capsule
                   Company Elanco US
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
DL-alpha-tocopherol DIG Info Presenilin 1 (EC50 > 100000 nM) [6]
Polyoxyl 35 castor oil DIG Info Cholesterol 25-hydroxylase (EC50 = 1.1 uM) [8]
             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
Sorbitol; Glycerin; Polyethylene glycol 400; Polyoxyl 40 hydrogenated castor oil; Tocophersolan; Alcohol; Gelatin
                   Dosage Form Oral Capsule
                   Company Eon Labs
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Hydrogenated polyoxyl 40 castor oil DIG Info Cytochrome P450 2C9 (IC50 = 30 uM) [7]
Tocophersolan DIG Info Albendazole monooxygenase (EC50 = 28.3 uM) [8]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [4]
             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
Sorbitol; Ferric oxide red; Glycerin; Titanium dioxide; Alcohol; Castor oil; Corn oil; Gelatin; Olive oil
                   Dosage Form Oral Capsule
                   Company Novartis Pharmaceuticals Corporation
          Cyclosporin A 50 mg capsule 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
Glycine; Alpha.-tocopherol, dl-; Fd&c blue no. 2; Sorbitol; Ferric oxide yellow; Glycerin; Propylene glycol; Titanium dioxide; Polyoxyl 40 hydrogenated castor oil; Alcohol; Aluminum oxide; Gelatin; Polyglyceryl-10 oleate; Polyglyceryl-3 oleate; Shellac
                   Dosage Form Oral Capsule
                   Company IVAX Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Aminoethanoic acid DIG Info Glycine type-1 transporter (IC50 = 31600 nM) [5]
DL-alpha-tocopherol DIG Info Presenilin 1 (EC50 > 100000 nM) [6]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Hydrogenated polyoxyl 40 castor oil DIG Info Cytochrome P450 2C9 (IC50 = 30 uM) [7]
             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
Sorbitan monooleate; Fd&c blue no. 2; Propylene glycol; Titanium dioxide; Polyoxyl 35 castor oil; Polysorbate 80; Alcohol; Gelatin; Polyethylene glycols
                   Dosage Form Oral Capsule
                   Company AbbVie
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Polyoxyl 35 castor oil DIG Info Cholesterol 25-hydroxylase (EC50 = 1.1 uM) [8]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
             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
Glycine; Alpha.-tocopherol, dl-; Sorbitol; Ferric oxide yellow; Glycerin; Titanium dioxide; Polyoxyl 40 hydrogenated castor oil; Alcohol; Gelatin; Polyglyceryl-10 oleate; Polyglyceryl-3 oleate
                   Dosage Form Oral Capsule
                   Company Teva Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Aminoethanoic acid DIG Info Glycine type-1 transporter (IC50 = 31600 nM) [5]
DL-alpha-tocopherol DIG Info Presenilin 1 (EC50 > 100000 nM) [6]
Hydrogenated polyoxyl 40 castor oil DIG Info Cytochrome P450 2C9 (IC50 = 30 uM) [7]
             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
Alpha.-tocopherol, dl-; Polyoxyl 35 castor oil; Alcohol; Corn oil; Polyethylene glycols
                   Dosage Form Oral Capsule
                   Company Elanco US
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
DL-alpha-tocopherol DIG Info Presenilin 1 (EC50 > 100000 nM) [6]
Polyoxyl 35 castor oil DIG Info Cholesterol 25-hydroxylase (EC50 = 1.1 uM) [8]
          Cyclosporin A 10 mg capsule 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
Alpha.-tocopherol, dl-; Polyoxyl 35 castor oil; Alcohol; Corn oil; Polyethylene glycols
                   Dosage Form Oral Capsule
                   Company Elanco US
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
DL-alpha-tocopherol DIG Info Presenilin 1 (EC50 > 100000 nM) [6]
Polyoxyl 35 castor oil DIG Info Cholesterol 25-hydroxylase (EC50 = 1.1 uM) [8]
          Cyclosporine 25mg capsule 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
Alcohol; Corn Oil-Mono-Di-Triglycerides; Polyoxyl 40 Hydrogenated Castor Oil Nf; Dl-tocopherol; Gelatin Nf; Glycerol; Iron Oxide Black; Propylene Glycol; Titanium Dioxide; Carmine
                   Dosage Form Capsule
                   Company Novartis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Triolein DIG Info Oleamide hydrolase 1 (IC50 = 11000 nM) [12]
DL-alpha-tocopherol DIG Info Presenilin 1 (EC50 > 100000 nM) [6]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Gelatin DIG Info Mephenytoin 4-hydroxylase (EC50 = 20.5 uM) [8]
Hydrogenated polyoxyl 40 castor oil DIG Info Cytochrome P450 2C9 (IC50 = 30 uM) [7]
Carmine DIG Info Solute carrier SLCO2B1 (Inhibition ratio = 29.4 %) [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
Alcohol; Corn Oil; Gelatin; Iron Oxide Red; Linoleoyl Macrogolglycerides; Sorbitol; Titanium Dioxide; Glycerol; Iron Oxide Yellow
                   Dosage Form Capsule
                   Company Novartis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Triolein DIG Info Oleamide hydrolase 1 (IC50 = 11000 nM) [12]
Gelatin DIG Info Mephenytoin 4-hydroxylase (EC50 = 20.5 uM) [8]
          Cyclosporine 50mg/ml injectable 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
Cremophor El; Polyoxyethylated Castor Oil; Alcohol; Nitrogen; Sodium Chloride; Dextrose
                   Dosage Form Injectable
                   Company Novartis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polyoxyl 35 castor oil DIG Info Cholesterol 25-hydroxylase (EC50 = 1.1 uM) [8]
          Cyclosporine 100mg/ml solution 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
Alcohol; Ph; Helv; ; Olive Oil; Ph; Helv; Labrafil M 1944 Cs; Polyoxyethylated Oleic Glycerides
                   Dosage Form Solution
                   Company Novartis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Glyceryl monooleate DIG Info Diacylglycerol kinase alpha (Ki = 91000 nM) [13]
References
1 FDA label for approved cyclosporin A from the official website of the U.S. Food and Drug Administration.
2 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
3 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.
4 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
5 Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: development of a potent and CNS penetrant [3.1.0]-based lead. Bioorg Med Chem Lett. 2014 Feb 15; 24(4):1067-70.
6 Membrane anchoring -secretase modulators with terpene-derived moieties. Bioorg Med Chem Lett. 2013 Jul 1; 23(13):3852-6.
7 Effects of non-ionic surfactants on cytochrome P450-mediated metabolism in vitro. Eur J Pharm Biopharm. 2011 May;78(1):166-72.
8 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
9 Reviewing Hit Discovery Literature for Difficult Targets: Glutathione Transferase Omega-1 as an Example. J Med Chem. 2018 Sep 13; 61(17):7448-7470.
10 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.
11 An Agonist Radioligand for the Proinflammatory Lipid-Activated G Protein-Coupled Receptor GPR84 Providing Structural Insights. J Med Chem. 2020 Mar 12; 63(5):2391-2410.
12 Structure-activity relationship of a series of inhibitors of monoacylglycerol hydrolysis--comparison with effects upon fatty acid amide hydrolase. J Med Chem. 2007 Oct 4; 50(20):5012-23.
13 Identification of a novel DGKalpha inhibitor for XLP-1 therapy by virtual screening. Eur J Med Chem. 2019; 164:378-390.

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