DT-Web

DB01070 - Dihydrotachysterol


Identification
Name Dihydrotachysterol
Accession Number DB01070 (APRD00143)
Type small molecule
Description A vitamin D that can be regarded as a reduction product of vitamin D2. [PubChem]
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 398.6642
Groups approved
Monoisotopic Weight 398.354866094
Pharmacology
Indication Used for the prevention and treatment of rickets or osteomalacia, and to manage hypocalcemia associated with hypoparathyroidism or pseudohypoparathyroidism. Also used for the treatment of vitamin D dependent rickets, rickets or osteomalacia secondary to long-term high dose anticonvulsant therapy, early renal osteodystrophy, osteoporosis (in conjunction with calcium), and hypophosphatemia associated with Fanconi syndrome (with treatment of acidosis).
Mechanism of action Once hydroxylated to 25-hydroxydihydrotachysterol, the modified drug binds to the vitamin D receptor. The bound form of the vitamin D receptor serves as a transcriptional regulator of bone matrix proteins, inducing the expression of osteocalcin and suppressing synthesis of type I collagen. Vitamin D (when bound to the vitamin D receptor)stimulates the expression of a number of proteins involved in transporting calcium from the lumen of the intestine, across the epithelial cells and into blood. This stimulates intestinal calcium absorption and increases renal phosphate excretion. These are functions that are normally carried out by the parathyroid hormone.
Absorption Not Available
Protein binding >99%
Biotransformation Not Available
Route of elimination Not Available
Toxicity Toxicity associated with dihydrotachysterol is similar to that seen with large doses of vitamin D.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


Vitamin D3 receptor
Name Vitamin D3 receptor
Gene Name VDR
Pharmacological action yes
Actions agonist
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
  • Qaw F, Calverley MJ, Schroeder NJ, Trafford DJ, Makin HL, Jones G: In vivo metabolism of the vitamin D analog, dihydrotachysterol. Evidence for formation of 1 alpha,25- and 1 beta,25-dihydroxy-dihydrotachysterol metabolites and studies of their biological activity. J Biol Chem. 1993 Jan 5;268(1):282-92. - Pubmed
  • Qaw FS, Makin HL, Jones G: Metabolism of 25-hydroxydihydrotachysterol3 in bone cells in vitro. Steroids. 1992 May;57(5):236-43. - Pubmed
  • Gallagher JC, Sai AJ: Vitamin D insufficiency, deficiency, and bone health. J Clin Endocrinol Metab. 2010 Jun;95(6):2630-3. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 0.941

Predictions


Id Partner name Gene Name Score
3997 Cytochrome P450 24A1, mitochondrial CYP24A1 0.1823
493 25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial CYP27B1 0.1168
6891 Mediator of RNA polymerase II transcription subunit 1 MED1 0.0935
6228 Nuclear receptor coactivator 1 NCOA1 0.0897
1992 Vitamin D-binding protein GC 0.0578
581 Cytochrome P450 2R1 CYP2R1 0.0377
606 Cytochrome P450 27, mitochondrial CYP27A1 0.0339
4512 Cytochrome P450 3A4 CYP3A4 0.0314
1757 Myeloperoxidase MPO 0.0248
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0216
6182 Cytochrome P450 2J2 CYP2J2 0.0079
6017 Cholesterol side-chain cleavage enzyme, mitochondrial CYP11A1 0.006
6024 Cytochrome P450 1A1 CYP1A1 0.0041
6030 Cytochrome P450 2B6 CYP2B6 0.0039
4924 Cytochrome P450 2C8 CYP2C8 0.0036
6016 Cytochrome P450 2C19 CYP2C19 0.0034
4757 Cytochrome P450 2C9 CYP2C9 0.0033
4119 Cytochrome P450 2D6 CYP2D6 0.0032
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