Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00435)
Name
Milnacipran
Synonyms    Click to Show/Hide the Synonyms of This API
Milnacipran; 92623-85-3; Milnacipranum [Latin]; UNII-ES1O38J3C4; Milnacipran HCl; F 2207; (1R,2S)-2-(aminomethyl)-N,N-diethyl-1-phenylcyclopropane-1-carboxamide; 96847-55-1; ES1O38J3C4; (+-)-Milnacipran; 101152-94-7 (HCl); Milnacipranum; Milnace; Dextromilnacipran; (1R,2S)-2-(aminomethyl)-N,N-diethyl-1-phenylcyclopropanecarboxamide; (-)-milnacipran; (1R,2S)-2-(aminomethyl)-N,N-diethyl-1-phenylcyclopropane-1-carboxamide hydrochloride; Milnacipran [INN:BAN]; (?)-Milnacipran; Milnacipran (INN); Cyclopropanecarboxamide, 2-(aminomethyl)-N,N-diethyl-1-phenyl-, cis-(+-)-; SCHEMBL8099; CHEMBL252923; DTXSID3048287; BDBM86420; CHEBI:94468; ZINC14037; HY-B0168; (+-)-cis-2-(Aminomethyl)-N,N-diethyl-1-phenylcyclopropanecarboxamide; NCGC00165825-01; CAS_92623-85-3; D08222; AB00640027_06; 623M853; Q421058; UNII-G56VK1HF36 component GJJFMKBJSRMPLA-HIFRSBDPSA-N; (1R,2S)-2-(aminomethyl)-N,N-diethyl-1-phenyl-cyclopropane-1-carboxamide
Clinical Status
Approved
Disease Indication Asperger syndrome ICD-11: 6A02 [1]
PubChem CID
65833
Formula
C15H22N2O
Canonical SMILES
CCN(CC)C(=O)[C@@]1(C[C@@H]1CN)C2=CC=CC=C2
InChI
1S/C15H22N2O/c1-3-17(4-2)14(18)15(10-13(15)11-16)12-8-6-5-7-9-12/h5-9,13H,3-4,10-11,16H2,1-2H3/t13-,15+/m1/s1
InChIKey
GJJFMKBJSRMPLA-HIFRSBDPSA-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=65833"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 246.35 Topological Polar Surface Area 46.3
XlogP 1.4 Complexity 295
Heavy Atom Count 18 Rotatable Bond Count 5
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 2
Full List of Drug Formulations (DFMs) Containing This API
          Milnacipran 50 mg tablet Click to Show/Hide the Full List of Formulation(s):          5 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 blue no. 1; Fd&c blue no. 2; Fd&c yellow no. 5; Magnesium stearate; Dibasic calcium phosphate dihydrate; Talc; Titanium dioxide; Povidone; Silicon dioxide; Carboxymethylcellulose calcium; Hypromelloses; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company Stat Rx USA
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [2]
Hydrazine yellow DIG Info GABA(A) receptor alpha-1 (IC50 = 13 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
Fd&c blue no. 1; Fd&c blue no. 2; Fd&c yellow no. 5; Magnesium stearate; Dibasic calcium phosphate dihydrate; Talc; Titanium dioxide; Povidone; Silicon dioxide; Carboxymethylcellulose calcium; Hypromelloses; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company Rebel Distributors
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [2]
Hydrazine yellow DIG Info GABA(A) receptor alpha-1 (IC50 = 13 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
Fd&c blue no. 1; Fd&c blue no. 2; Fd&c yellow no. 5; Magnesium stearate; Dibasic calcium phosphate dihydrate; Talc; Titanium dioxide; Povidone; Carboxymethylcellulose calcium; Colloidal silicon dioxide; Hypromelloses; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company Lake Eire Medical & Surgical Supply DBA Quality Care Products; Physicians Total Care
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [2]
Hydrazine yellow DIG Info GABA(A) receptor alpha-1 (IC50 = 13 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
Magnesium stearate; Calcium phosphate, dibasic, dihydrate; Talc; Titanium dioxide; Polyvinyl alcohol; Povidone; Silicon dioxide; Carboxymethylcellulose calcium; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Allergan
                   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) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
Magnesium stearate; Dibasic calcium phosphate dihydrate; Talc; Titanium dioxide; Silicon dioxide; Carboxymethylcellulose calcium; Polyethylene glycol, unspecified; Polyvinyl alcohol, unspecified; Povidone, unspecified
                   Dosage Form Oral Tablet
                   Company Cardinal Health
                   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) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
          Milnacipran 100 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 red no. 40; Magnesium stearate; Calcium phosphate, dibasic, dihydrate; Talc; Titanium dioxide; Polyvinyl alcohol; Povidone; Silicon dioxide; Carboxymethylcellulose calcium; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Allergan
                   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) [3]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [2]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
Fd&c blue no. 1; Magnesium stearate; Dibasic calcium phosphate dihydrate; Talc; Titanium dioxide; Povidone; Silicon dioxide; Carboxymethylcellulose calcium; Hypromelloses; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company Stat Rx USA
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [2]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
Fd&c blue no. 1; Magnesium stearate; Dibasic calcium phosphate dihydrate; Talc; Titanium dioxide; Povidone; Carboxymethylcellulose calcium; Colloidal silicon dioxide; Hypromelloses; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company Physicians Total Care
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [2]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
          Milnacipran 12.5 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
Fd&c blue no. 2; Magnesium stearate; Calcium phosphate, dibasic, dihydrate; Talc; Titanium dioxide; Polyvinyl alcohol; Povidone; Silicon dioxide; Carboxymethylcellulose calcium; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Allergan
                   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) [3]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
          Milnacipran 25 mg tablet Click to Show/Hide the Full List of Formulation(s):          5 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
Magnesium stearate; Calcium phosphate, dibasic, dihydrate; Talc; Titanium dioxide; Polyvinyl alcohol; Povidone; Silicon dioxide; Carboxymethylcellulose calcium; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Allergan
                   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) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [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; Dibasic calcium phosphate dihydrate; Talc; Titanium dioxide; Povidone; Silicon dioxide; Carboxymethylcellulose calcium; Hypromelloses; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company Stat Rx USA
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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; Dibasic calcium phosphate dihydrate; Talc; Titanium dioxide; Polyethylene glycol 400; Povidone; Carboxymethylcellulose calcium; Colloidal silicon dioxide; 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
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [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
Magnesium stearate; Dibasic calcium phosphate dihydrate; Talc; Titanium dioxide; Povidone; Silicon dioxide; Carboxymethylcellulose calcium; Hypromelloses; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company Rebel Distributors
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
Magnesium stearate; Dibasic calcium phosphate dihydrate; Talc; Titanium dioxide; Silicon dioxide; Carboxymethylcellulose calcium; Polyethylene glycol, unspecified; Polyvinyl alcohol, unspecified; Povidone, unspecified
                   Dosage Form Oral Tablet
                   Company 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) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
References
1 FDA label for approved milnacipran 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 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
5 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
6 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.

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