Delving into the Latest Updates on Becocalcidiol with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Becocalcidiol (USAN/INN)

+ [3]

Target

VDR

Mechanism

VDR agonists(Vitamin D receptor agonists)

Therapeutic Areas

Immune System DiseasesSkin and Musculoskeletal Diseases

Active Indication-

Inactive Indication

Plaque psoriasis

Originator Organization

QuatRx Pharmaceuticals Co.

Active Organization-

Inactive Organization

QuatRx Pharmaceuticals Co.

Deltanoid Pharmaceuticals, Inc.

Drug Highest PhasePendingPhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC23H36O2

InChIKeyQSLUXQQUPXBIHH-YHSKWIAJSA-N

CAS Registry524067-21-8

Low doses of topically administered vitamin D analogs have been shown to have an anti-psoriatic effect without the risk of hypercalcemia. Calcipotriol, the most thoroughly studied of the vitamin D analogs, was first approved in Europe in the early 1990s. It has been shown to be comparable or slightly more effective than class II corticosteroid ointments. However, patients had reduced levels of parathyroid hormone; mean serum and urine calcium were increased during treatment and hypercalciuria was observed. These effects were reversible with discontinuation of therapy. Thus, while calcipotriol ointment was shown to be effective, the potential for alterations in calcium homeostasis have limited its use to 100 g of ointment per week (0.5 mg calcipotriol/week). Work has continued on the creation of new vitamin D analogs, such as COL-121, with the intent of eliminating the adverse effects of hypercalcemia and hypercalciuria with a compound that is more stable and more easily administered.

Start Date01 Jan 2008

Sponsor / Collaborator

Deltanoid Pharmaceuticals, Inc.

NCT00373516 / CompletedPhase 2

A Multi-Center, Randomized, Double-Blind, Parallel-Group, Vehicle-Controlled, Study of the Safety and Efficacy of Two Dosing Regimens of QRX-101 (Becocalcidiol) Ointment in the Treatment of Plaque-Type Psoriasis

The purpose of this study is to evaluate the efficacy and safety of two dosing regimens of QRX-101 ointment (75 mcg/g QD and 75mcg/g BID) in the treatment of plaque-type psoriasis when applied topically twice daily for 8 weeks

Start Date01 Sep 2004

Sponsor / Collaborator

QuatRx Pharmaceuticals Co.

100 Clinical Results associated with Becocalcidiol

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100 Translational Medicine associated with Becocalcidiol

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100 Patents (Medical) associated with Becocalcidiol

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10

Literatures (Medical) associated with Becocalcidiol

12 Apr 2011·Journal of Pharmacy and PharmacologyQ3 · MEDICINE

Invariable susceptibility to blockade by nifedipine of vasoconstriction to various α2-adrenoceptor agonists in pithed rats

Q3 · MEDICINE

Article

Author: Wilffert, Bob ; De Jonge, Adriaan ; Zwieten, Pieter A van ; Mathy, Marie-Jeanne ; Thoolen, Martin J M C ; Timmermans, Pieter B M W M

AbstractThe sensitivity of the increase in diastolic pressure brought about by the selective agonists of α2-adrenoceptors, B-HT 920, B-HT 933, xylazine, UK-14,304, M-7, TL-99 and DP-6, 7-ADTN in pithed normotensive rats to blockade by the calcium entry inhibitor nifedipine has been investigated. To exclude any participation of vascular α1- and β2-adrenoceptors, as well as cardiac β1-adrenoceptors, in the pressor responses, the study was made after treatment of the pithed rats with prazosin (0·1 mg kg−1) and (-)-propranol (1 mg kg−1). Without exception, the preferential agonists of α2-adrenoceptors elicited vasoconstrictor responses which were susceptible to inhibition by nifedipine (0·03–1 mg kg−1) in a dose-dependent manner regardless of the differences in intrinsic activity of the compounds. The pressor activity was almost completely abolished after 1 mg kg−1 of nifedipine. The results show that vasoconstriction induced in pithed rats by various selective stimulating agents of postjunctional vascular α2-adrenoceptors is invariably and equally sensitive to attenuation by nifedipine. This susceptibility of α2-adrenoceptor-mediated vasoconstriction to impairment by blockade of calcium entry is not dependent on the nature, the potency or the efficacy of the agonist.

01 Oct 2010·ThyroidQ1 · MEDICINE

Thyroid Cancer Resistance to Vitamin D Receptor Activation Is Associated with 24-Hydroxylase Levels But Not theffFokI Polymorphism

Q1 · MEDICINE

Article

Author: Crees, Zachary ; Sharma, Vibha ; Kerege, Anna ; Klopper, Joshua P. ; Fretwell, Deborah

BACKGROUNDThe vitamin D receptor (VDR) has been studied as a novel target for cancer therapy in many tissue types as VDR ligands decrease cell proliferation in vitro and decrease tumor growth in vivo in sensitive cells. The objective of this study was to analyze the response to VDR agonist therapy in a panel of validated thyroid cancer cells and assess genetic markers predicting sensitivity and resistance to calcitriol and the noncalcemic analog DP006.METHODSThyroid cancer cell lines were analyzed for VDR and RXR protein by Western blot. Cell growth after VDR agonist treatment (calcitriol or DP006) was assessed after 6 days of treatment by viable cell assay. To investigate calcitriol/DP006 resistance in VDR-expressing cells, the VDR was sequenced and 1-α and 24-hydroxylase mRNA expression was assessed.RESULTSVDR protein was variably expressed in the thyroid cancer cell lines and its presence was not sufficient for decreased viable cell count in response to calcitriol or DP006. The most sensitive cells (TPC1) have an ff FokI VDR polymorphism and the most resistant cells (HTh7 and 8505C) have an FF FokI VDR. This is a unique finding given that the balance of the literature of VDR polymorphisms describes an association of the ff FokI polymorphism with cancer risk and/or decreased VDR transactivation. 1-α and 24-hydroxylase mRNA expression before and after VDR agonist therapy was examined. 1-α-Hydroxylase levels did not change after calcitriol treatment. However, we found that higher baseline 24-hydroxylase levels and/or lower stimulation of 24-hydroxylase levels after calcitriol treatment were associated with relative resistance to calcitriol/DP006.CONCLUSIONSThe VDR represents a novel therapeutic target in poorly differentiated thyroid cancer; however, the efficacy of VDR agonist therapy to decrease viable thyroid cancer cell count cannot be predicted solely on the presence of the VDR. The FF FokI VDR genotype and high baseline 24-hydroxylase levels were associated with relative resistance to calcitriol and DP006. Therefore, identifiable markers of sensitivity or resistance to VDR agonist therapy may allow for a personalized use of these agents in poorly differentiated thyroid cancer.

01 Nov 2008·SteroidsQ4 · MEDICINE

2-Methylene-19-nor-20(S)-1α-hydroxy-bishomopregnacalciferol [20(S)-2MbisP], an analog of vitamin D3 [1,25(OH)2D3], does not stimulate intestinal phosphate absorption at levels previously shown to suppress parathyroid hormone

Q4 · MEDICINE

Article

Author: Hector F. DeLuca ; Katie B. Williams

Chronic kidney disease results in a reduction in 1,25-dihydroxyvitamin D3 (1,25(OH)2D3) synthesis and an accumulation of phosphorus in the blood, leading to secondary hyperparathyroidism and renal osteodystrophy. Vitamin D analogs that retain the ability to suppress PTH but that are less calcemic and phosphatemic than the native hormone are preferred therapies for secondary hyperparathyroidism. However, even the most favored analog currently approved for the treatment of chronic kidney disease patients, i.e. 1,25-dihydroxy-19-nor-vitamin D2 (19-nor-D2, Zemplar), still retains some ability to stimulate intestinal absorption of calcium and phosphate. A recently described analog of vitamin D3, 2-methylene-19-nor-20(S)-1alpha-hydroxy-bishomopregnacalciferol [20(S)-2MbisP], suppresses PTH levels, but is unable to stimulate intestinal calcium absorption or bone resorption in rats. The present study shows that 20(S)-2MbisP is unable to stimulate intestinal phosphate absorption at levels known to suppress PTH secretion. Further, 19-nor-vitamin D2 under the same circumstances does stimulate phosphate absorption. Thus, 2MbisP has significant potential in the management of secondary hyperparathyroidism of renal failure.

100 Deals associated with Becocalcidiol

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External Link

KEGG	Wiki	ATC	Drug Bank
D08868	-	-	DB04891

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Plaque psoriasis	Phase 2	US	QuatRx Pharmaceuticals Co.	01 Sep 2004

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00373516 (Pubmed \| Br J Dermatol)	Phase 2	Psoriasis vulgaris	-	Placebo	aaiackepcq(wlgjjnwfjb): P-Value = 0.002	Positive	01 Aug 2007
				Becocalcidiol 75 microg g(-1) twice daily