Paricalcitol Chemical Properties

Boiling point:

564.8±50.0 °C(Predicted)

Density 

1.121±0.06 g/cm3(Predicted)

Flash point:

14℃

storage temp. 

Store at -20°C,unstable in solution, ready to use.

solubility 

DMSO : 100 mg/mL (240.02 mM; Need ultrasonic)Ethanol : 12.5 mg/mL (30.00 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)

pka

14.34±0.40(Predicted)

form 

Solid

color 

White to off-white

InChIKey

BPKAHTKRCLCHEA-UBFJEZKGSA-N

SMILES

C[C@]12CCC/C(=C\C=C3C[C@@H](O)C[C@H](O)C3)/[C@]1([H])CC[C@]2([H])[C@H](C)/C=C/[C@H](C)C(O)(C)C |&1:1,10,13,16,20,22,26,r|

CAS DataBase Reference

131918-61-1(CAS DataBase Reference)

Safety Information

RIDADR 

UN1170 - class 3 - PG 2 - Ethanol, solution

HS Code 

2936299055

Hazardous Substances Data

131918-61-1(Hazardous Substances Data)

Paricalcitol Usage And Synthesis

Description

Paricalcitol was launched as Zemplar in the US for the prevention and treatment of secondary hyperthyroidism associated with chronic renal failure. Paricalcitol is a synthetic vitamin D2, namely a novel 1-alpha-hydroxy-19-noranalogue in which the ring A exocyclic methylene group, typical of all vitamin D systems, has been replaced by two hydrogen atoms. Paricalcitol is the first vitamin D analogue marketed for this indication. In patients with chronic renal failure, Paricalcitol appreciably reduced levels of parathyroid hormone (PTH) without a significant difference in the incidence rate for hypercalcemia or hyperphosphatemia when compared with placebo.

Description

Paricalcitol is a synthetic 1,25-dihydroxy vitamin D₂ analog. As vitamin D deficiency, associated with chronic kidney disease, leads to an increase in parathyroid hormone (secondary hyperparathyroidism), paricalcitol is used in renal patients to block parathyroid hormone overproduction. Vitamin D deficiency is also a risk factor in cancer, cardiovascular disease, hypertension, and diabetes, and paricalcitol may have applications in those contexts as well.

Chemical Properties

White Solid

Originator

Abbott (US)

Uses

Antihyperparathyriod

Uses

1,25-Dihydroxy vitamin D2 is a potent agonist of the vitamin D receptor. Paricalcitol is a synthetic 1,25-dihydroxy vitamin D2 analog. As vitamin D deficiency, associated with chronic kidney disease, leads to an increase in parathyroid hormone (secondary hyperparathyroidism), paricalcitol is used in renal patients to block parathyroid hormone overproduction. Vitamin D deficiency is also a risk factor in cancer, cardiovascular disease, hypertension, and diabetes, and paricalcitol may have applications in those contexts as well.

Uses

Synthetic analog of vitamin D. Antihyperparathyroid.

Definition

ChEBI: Paricalcitol is a seco-cholestane and a hydroxy seco-steroid. It has a role as an antiparathyroid drug. It is functionally related to a vitamin D2.

brand name

Zemplar (Abbott).

Clinical Use

Vitamin D analogue:
Treatment and prevention of secondary hyperparathyroidism associated with chronic renal failure

Metabolism

Extensively metabolised via hepatic and non-hepatic pathways to form two relatively inactive metabolites. After oral administration of 3 H-paricalcitol, only about 2% of the dose was eliminated unchanged in the faeces, and no parent drug found in the urine.
Approximately 70% of the radioactivity was eliminated in the faeces and 18% was recovered in the urine. Most of the systemic exposure was from the parent drug.

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