Delving into the Latest Updates on DP-001 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

VDR

Mechanism

VDR agonists(Vitamin D receptor agonists)

Therapeutic Areas

Endocrinology and Metabolic DiseaseSkin and Musculoskeletal DiseasesUrogenital Diseases

Active Indication-

Inactive Indication

Hyperparathyroidism, SecondaryKidney Failure, ChronicOsteoporosis+ [1]

Originator Organization

University of Wisconsin Madison

Active Organization-

Inactive Organization

University of Wisconsin Madison

Deltanoid Pharmaceuticals, Inc.

Pfizer Inc.

Drug Highest PhasePendingPhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC27H44O3

InChIKeyUHMPCVGLSKFXHR-NAQZCRMNSA-N

CAS Registry213250-70-5

This is an open-label, dose-ranging study of the vitamin D analog DP001 in patients with end-stage renal disease (ESRD). The primary goals of this 4-week Phase 2A study are to identify an appropriate starting dose of DP001 to be used in subsequent studies in this population and for evaluation of pharmacokinetics of DP001 in ESRD patients.

Start Date01 Aug 2012

Sponsor / Collaborator

Deltanoid Pharmaceuticals, Inc.

NCT00715676 / CompletedPhase 2

A Phase 2, Double-blind, Randomized, Placebo-Controlled, Daily-dose, Proof-of-concept Study of a Vitamin D Compound in Postmenopausal Women With Osteopenia

This study will evaluate the effect of a 1-year administration of the vitamin D analog 2-methylene-19-nor-(20S)-1alpha, 25-dihydroxyvitamin D3 (DP001) on bone mineral density (BMD), safety, and tolerability.

Start Date01 Mar 2007

Sponsor / Collaborator

Deltanoid Pharmaceuticals, Inc.

100 Clinical Results associated with DP-001

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100 Translational Medicine associated with DP-001

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100 Patents (Medical) associated with DP-001

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24

Literatures (Medical) associated with DP-001

01 Dec 2020·Journal of Bone and Mineral ResearchQ1 · MEDICINE

A New 1,25 Dihydroxy Vitamin D Analog with Strong Bone Anabolic Activity in OVX Rats with Little or no Bone Resorptive Activity

Q1 · MEDICINE

Article

Author: DeLuca, Hector F ; Plum, Lori A ; Zella, Julia ; Clagett-Dame, Margaret

ABSTRACTA new 1α,25-dihydroxy vitamin D3 analog (2-methylene-22(E)-(24R)-22-dehydro-1α,24,25-trihydroxy-19-norvitamin D3 or WT-51) has been tested as a possible therapeutic for osteoporosis. It is 1/10th as active as 1,25(OH)2D3 in binding affinity for the vitamin D receptor but is at least 200 times more active than 1,25(OH)2D3 and equal to that of 2MD (2-methylene-19-nor-(20S)-1α,25(OH)2D3, an analog previously tested in postmenopausal women), in supporting bone formation by isolated osteoblasts in culture. However, in contrast to 2MD, it is virtually inactive on bone resorption in vivo. WT-51 markedly increased bone mass (lumbar and femur) in ovariectomized (OVX) female rats. Further, bone strength tested by the three-point bending system is significantly increased by WT-51. Thus, WT-51 is an attractive candidate for the treatment of postmenopausal osteoporosis. © 2019 American Society for Bone and Mineral Research.

01 Dec 2017·Drugs in R&DQ4 · MEDICINE

Pharmacokinetics of a New Oral Vitamin D Receptor Activator (2-Methylene-19-Nor-(20S)-1α,25-Dihydroxyvitamin D3) in Patients with Chronic Kidney Disease and Secondary Hyperparathyroidism on Hemodialysis

Q4 · MEDICINE

ArticleOA

Author: Blaser, William J ; Zhu, Jinge G ; Plum, Lori A ; Clagett-Dame, Margaret ; Coyne, Daniel W ; Pandey, Richa ; Bedale, Wendy ; DeLuca, Hector F ; Zella, Julia B

BACKGROUND2-Methylene-19-nor-(20S)-1α,25-dihydroxyvitamin D₃ (DP001 or 2MD) is a novel, potent 1α-hydroxylated vitamin D analog that binds to the vitamin D receptor and suppresses parathyroid hormone synthesis and secretion with potential for an improved safety profile compared to existing active vitamin D analogs. The purpose of this study was to evaluate the pharmacokinetics of DP001 given orally after hemodialysis.METHODSDP001 (550 ng) was given orally to 11 hemodialysis patients with secondary hyperparathyroidism after each dialysis session (3 times/week) for 4 weeks. Pharmacokinetic analyses were performed after the first and final dose.RESULTSAfter the first and final dose, the half-life of DP001 was similar (55.8 ± 13.0 and 50.8 ± 8.2 h, respectively). At 4 weeks, the time to maximum plasma concentration was 4.0 ± 0.8 h, with a concentration maximum of 3.4 ± 0.3 pg/mL. The area under the curve (0 to infinity) after the final dose was 204.3 ± 23.9 pg h/mL, and apparent volume of distribution was 2.03 ± 0.22 L/kg. At week 4, mean intact parathyroid hormone was suppressed 33% from the baseline (pre-dose) value (313 ± 52 vs 462 ± 39 pg/mL, respectively). No clinically significant changes from baseline values were found for vital signs, electrocardiogram measurements, or other laboratory parameters, including serum calcium and phosphorus.CONCLUSIONSIn hemodialysis patients, DP001 has a longer half-life than existing vitamin D therapies and enables control of parathyroid hormone when administered every 2-3 days on the day of dialysis. It is effective at a lower concentration maximum and area under the curve than other clinically available vitamin D compounds. DP001 may represent a therapeutic improvement over existing compounds due to rapid and extensive distribution to its target and its long half-life enabling sustained parathyroid hormone suppression. These studies support further evaluation of DP001 in longer-term treatment of secondary hyperparathyroidism.

01 Jan 2017·American Journal of NephrologyQ3 · MEDICINE

2MD (DP001), a Single Agent in the Management of Hemodialysis Patients: A Randomized Trial

Q3 · MEDICINE

Article

Author: Clagett-Dame, Margaret ; Blaser, William J. ; Zella, Julia B. ; DeLuca, Hector F. ; Knutson, Danielle C. ; Plum, Lori A. ; Thadhani, Ravi ; Buck, Raymond D.

Background: Vitamin D analogs and calcimimetics are used to manage secondary hyperparathyroidism (SHPT) in dialysis patients. DP001 is an oral vitamin D analog that suppresses parathyroid hormone (PTH) in uremic rats, osteopenic women, and hemodialysis patients. The safety and effectiveness of DP001 suppressing PTH in dialysis patients previously managed with active vitamin D with or without a calcimimetic are presented. Methods: A multicenter, randomized, double-blind study compared DP001 to placebo in hemodialysis patients with serum-intact PTH (iPTH) ≥300 pg/ml. The primary efficacy endpoint was the proportion of patients achieving 2 consecutive ≥30% decreases in iPTH levels during the 12 weeks of treatment. Calcium, phosphorus, calcium × phosphorus product and safety were also evaluated. The responses to DP001 were compared in patients previously treated with both active vitamin D and a calcimimetic to those previously on active vitamin D alone. Results: Sixty-two patients were randomized (n = 34 DP001; n = 28 placebo). At week 12, 78% of all DP001-treated patients and 7% of all placebo-treated patients achieved the primary endpoint (p < 0.0001); iPTH fell 45% in the DP001 group and increased 37% in the placebo group. No patient exceeded the safety threshold of 2 consecutively corrected serum calcium levels ≥11.0 mg/dl. Patients previously on cinacalcet plus active vitamin D also responded to DP001 (n = 10) resulting in a 55% decrease in iPTH, while those on placebo (n = 9) increased by 70%. Conclusion: DP001 safely and effectively suppressed iPTH in hemodialysis patients with SHPT that were previously managed with active vitamin D alone or with a calcimimetic (www.clinicaltrials.gov, NCT01922843).

100 Deals associated with DP-001

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Kidney Failure, Chronic	Phase 2	US	Deltanoid Pharmaceuticals, Inc.	01 Sep 2013
Hyperparathyroidism, Secondary	Phase 2	US	Deltanoid Pharmaceuticals, Inc.	01 Aug 2012
Osteoporosis	Phase 2	US	Deltanoid Pharmaceuticals, Inc.	01 Mar 2007
Osteoporosis, Postmenopausal	Phase 2	-	University of Wisconsin Madison	-
Osteoporosis, Postmenopausal	Phase 2	-	Pfizer Inc.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01922843 (2MD-7H-2B, Pubmed \| Am J Nephrol) Manual	Phase 2	Hyperparathyroidism, Secondary	62	2MD	(vxjdbhfwry) = qrsfzbgoci exnshockql (jtueahoxgr ) View more	Positive	01 Jan 2017
				Placebo	(vxjdbhfwry) = iyyftsjsfm exnshockql (jtueahoxgr ) View more
NCT00715676 (2MD-3H-2B, CTgov)	Phase 2	Osteoporosis	157	Placebo (Placebo)	lmfqmqehyf(hxpqmdofly) = yitzostpap gjggufmytc (bhhywfdahf, usplvsfjcl - wughdzdlof) View more	-	11 Jan 2010
				DP001 (220 ng DP001)	lmfqmqehyf(hxpqmdofly) = opjtgoqbqf gjggufmytc (bhhywfdahf, uzvlgblcbq - nlrxsxohhl) View more