Identification
Name Prednicarbate
Accession Number DB01130 (APRD01197)
Type small molecule
Description Prednicarbate is a relatively new topical corticosteroid drug. It is similar in potency to hydrocortisone. It is used in the treatment of inflammatory skin diseases, such as atopic dermatitis. It has a favorable benefit-risk ratio, with an inflammatory action similar to that of a medium potency corticosteroid, but with a low potential to cause skin atrophy. The anti-inflammation action of corticosteroids is associated with the inhibition of the interleukin 1-alpha cytokine within keratinocytes. IL-1a is also found in fibroblasts, where it is responsible for proliferation, collagenase induction and IL-6 synthesis, which are related to skin thickness.
Structure
Categories (*)
Molecular Weight 488.5699
Groups approved
Monoisotopic Weight 488.241018128
Pharmacology
Indication For the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.
Mechanism of action In common with other topical corticosteroids, prednicarbate has anti-inflammatory, antipruritic, and vasoconstrictive properties. In general, the mechanism of the anti-inflammatory activity of topical steroids is unclear. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.
Absorption Absorbed systemically across the stratum corneum.
Protein binding Not Available
Biotransformation Primarily in skin
Route of elimination Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions Not Available
Glucocorticoid receptor
Name Glucocorticoid receptor
Gene Name NR3C1
Pharmacological action yes
Actions agonist
References
  • Boudinot FD, D'Ambrosio R, Jusko WJ: Receptor-mediated pharmacodynamics of prednisolone in the rat. J Pharmacokinet Biopharm. 1986 Oct;14(5):469-93. - Pubmed
  • Ikonomidis I, Tzortzis S, Lekakis J, Paraskevaidis I, Andreadou I, Nikolaou M, Kaplanoglou T, Katsimbri P, Skarantavos G, Soucacos P, Kremastinos DT: Lowering interleukin-1 activity with anakinra improves myocardial deformation in rheumatoid arthritis. Heart. 2009 Sep;95(18):1502-7. Epub 2009 May 28. - Pubmed
DTHybrid score 0.778
Id Partner name Gene Name Score
232 Corticosteroid-binding globulin SERPINA6 0.2409
4512 Cytochrome P450 3A4 CYP3A4 0.0775
469 Annexin A1 ANXA1 0.0385
1588 Multidrug resistance protein 1 ABCB1 0.0326
614 Progesterone receptor PGR 0.0223
737 Mineralocorticoid receptor NR3C2 0.0198
723 Cytosolic phospholipase A2 PLA2G4A 0.0179
146 Androgen receptor AR 0.0161
4118 Cytochrome P450 3A5 CYP3A5 0.0143
381 Prolactin receptor PRLR 0.0142
4924 Cytochrome P450 2C8 CYP2C8 0.0122
756 Sex hormone-binding globulin SHBG 0.0114
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0112
2751 Holliday junction ATP-dependent DNA helicase ruvB ruvB 0.0105
4755 Holliday junction ATP-dependent DNA helicase ruvB ruvB 0.0105
4615 Chain A, Red Copper Protein Nitrosocyanin NE0143 0.0093
6024 Cytochrome P450 1A1 CYP1A1 0.0084
3811 Cytochrome P450 19A1 CYP19A1 0.0083
6107 Cytochrome P450 3A7 CYP3A7 0.008
1758 GTPase HRas HRAS 0.0068
4119 Cytochrome P450 2D6 CYP2D6 0.0063
4604 Liver carboxylesterase 1 CES1 0.0061
4200 Cytochrome P450 1A2 CYP1A2 0.0061
6500 Phospholipase A2 PLA2G1B 0.006
136 Estrogen receptor ESR1 0.0052
3923 Cholinesterase BCHE 0.0049
5718 Cytochrome P450 2A6 CYP2A6 0.0048
364 Corticosteroid 11-beta-dehydrogenase isozyme 1 HSD11B1 0.0048
290 Prostaglandin G/H synthase 2 PTGS2 0.0048
2300 Lysozyme E 0.0047
3633 Lysozyme R 0.0047
5597 Lysozyme 17 0.0047
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0035
6016 Cytochrome P450 2C19 CYP2C19 0.0034
862 Multidrug resistance-associated protein 1 ABCC1 0.0031
587 Serum albumin ALB 0.003
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0028
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0028
84 Nuclear receptor 0B1 NR0B1 0.0023
380 Cytochrome P450 17A1 CYP17A1 0.0017
6031 Cytochrome P450 3A43 CYP3A43 0.0014
468 Cytochrome P450 4A11 CYP4A11 0.0014
6017 Cholesterol side-chain cleavage enzyme, mitochondrial CYP11A1 0.0013
1898 Cytochrome P450 1B1 CYP1B1 0.0011
776 Bile salt export pump ABCB11 0.0011
7 Nitric oxide synthase, inducible NOS2 0.0011
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.0009
6030 Cytochrome P450 2B6 CYP2B6 0.0008
6013 Cytochrome P450 2E1 CYP2E1 0.0008
4757 Cytochrome P450 2C9 CYP2C9 0.0007