Investigational Drug Details
| Drug ID: | D031 |
| Drug Name: | Ergocalciferol |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB00153 |
| DrugBank Description: | Ergocalciferol is an inactivated vitamin D analog.[A177526] It is a form of vitamin synthesized by some plants in the presence of UVB light.[T577] The production of ergocalciferol was impulsed by the identification of dietary deficiency, more specifically vitamin D, as the main causative agent for rickets. Impulsed by this research, ergocalciferol was isolated for the first time from yeast in 1931 and its structure was elucidated in 1932.[T580] Ergocalciferol is considered the first vitamin D analog and it differentiates from [cholecalciferol] in the presence of a double bond between C22 and C23 and the presence of a methyl group at C24. These modifications reduce the affinity of ergocalciferol to vitamin D binding protein which derives in faster clearance, limits its activation and alters its catabolism.[A177637] The first approved product containing ergocalciferol under the FDA records was developed by US Pharm Holdings and FDA approved in 1941.[L6058] |
| PubChem ID: | 5280793 |
| CasNo: | 50-14-6 |
| Repositioning for NAFLD: | Yes |
| SMILES: | CC(C)[C@@H](C)\C=C\[C@@H](C)[C@@]1([H])CC[C@@]2([H])\C(CCC[C@]12C)=C\C=C1\C[C@@H](O)CCC1=C |
| Structure: |
|
| InChiKey: | MECHNRXZTMCUDQ-RKHKHRCZSA-N |
| Molecular Weight: | 396.6484 |
| DrugBank Targets: | Vitamin D3 receptor; Voltage-dependent calcium channel |
| DrugBank MoA: | For its activity, ergocalciferol is required to be transformed to its major active circulating hydroxylated metabolite and transported to the target organs in order to bind to its target, the vitamin D receptor.[T580] The activation of the vitamin D receptor is part of the vitamin D endocrine system and it is described by the production of a change in the transcription rates of the vitamin D receptor target genes.[T580] The target genes in the DNA affected by the presence of ergocalciferol are called vitamin D response elements which are dependent on co-modulators.[A177637] The vitamin D receptor is a transcription factor and member of the steroid hormone nuclear receptor family. It presents a DNA binding domain (VDRE) that, when activated, recruits coregulatory complexes to regulate the genomic activity.[A177637] Additionally, ergocalciferol presents nongenomic effects such as the stimulation of intestinal calcium transport via transcaltachia.[A177637] |
| DrugBank Pharmacology: | After the activation of the vitamin D receptor, some of the biological changes produced by ergocalciferol include mobilization and accretion of calcium and phosphorus in the bone, absorption of calcium and phosphorus in the intestine, and reabsorption of calcium and phosphorus in the kidney.[T580] Some other effects known to be produced due to the presence of vitamin D are osteoblast formation, fetus development, induction of pancreatic function, induction of neural function, improvement of immune function, cellular growth and cellular differentiation.[T580] When compared to its vitamin D counterpart [cholecalciferol], ergocalciferol has been shown to present a reduced induction of calcidiol and hence, it is less potent.[A177529] Ergocalciferol supplementation in patients with end-stage renal disease has been shown to generate a significant benefit in lab parameters of bone and mineral metabolism as well as improvement in glycemic control, serum albumin levels and reduced levels of inflammatory markers.[A177526] |
| DrugBank Indication: | Ergocalciferol is indicated for the treatment of hypoparathyroidism, refractory rickets, and familial hypophosphatemia.[FDA label] Hypoparathyroidism is the result of inadequate parathyroid hormone production that occurs due to the presence of damage or removal of the parathyroid glands. This condition produces decreased calcium and increased phosphorus levels.[L6082] Rickets is a condition produced due to a deficiency in vitamin D, calcium or phosphorus. However, this condition can also be related to renal diseases. It is characterized to present weak or soft bones.[A177664] Familial hypophosphatemia is characterized by the impaired transport of phosphate and an altered vitamin D metabolism in the kidneys. The presence of this condition can derive in the presence of osteomalacia, bone softening and rickets.[L6085] |
| Targets: | |
| Therapeutic Category: | |
| Clinical Trial Progress: | |
| Latest Progress: |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0513 | NCT05491642 | PHASE1 | COMPLETED | NO | 2022-09-08 | 2023-05-17 | Details |
| L0586 | NCT04655027 | PHASE4 | COMPLETED | YES | 2021-02-22 | 2024-04-22 | Details |
| L1744 | NCT01986855 | PHASE3 | COMPLETED | YES | 2013-12-02 | 2018-09-10 | Details |
| L2208 | NCT00473330 | PHASE3 | COMPLETED | YES | 2007-06 | 2017-04-17 | Details |
| L2456 | NCT05140694 | PHASE4 | NOT_YET_RECRUITING | NO | 2023-12-01 | 2022-10-04 | Details |
| L2582 | NCT01022112 | PHASE2 | COMPLETED | YES | 2009-11 | 2014-06-05 | Details |
| L2648 | NCT04192292 | COMPLETED | NO | 2019-10-08 | 2021-03-04 | Details | |
| L3017 | NCT05943886 | PHASE1 | COMPLETED | NO | 2021-08-11 | 2023-07-17 | Details |
| L3024 | NCT01324739 | COMPLETED | NO | 2010-05 | 2011-03-29 | Details | |
| L3038 | NCT00162357 | PHASE4 | COMPLETED | NO | 2004-04 | 2011-04-15 | Details |
| L3429 | NCT03608163 | PHASE4 | UNKNOWN | NO | 2018-08-10 | 2023-03-17 | Details |
| L3598 | NCT01436201 | PHASE1 | COMPLETED | YES | 2011-09 | 2014-10-07 | Details |
| L5039 | NCT02462421 | PHASE4 | TERMINATED | YES | 2015-06-01 | 2022-08-02 | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Article ID | PMID | Source | Title |
|---|