Upacicalcet: Difference between revisions

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'''Upacicalcet''' is a novel [[pharmaceutical drug]] currently under development for the treatment of [[hyperparathyroidism]] and [[hypercalcemia]] associated with [[chronic kidney disease]] (CKD). It is a [[calcimimetic]] agent, designed to mimic the action of calcium on tissues, particularly the [[parathyroid gland]].
{{Short description|A calcimimetic drug used in the treatment of secondary hyperparathyroidism}}
{{Drugbox
| verifiedrevid = 123456789
| image = Upacicalcet.svg
| width = 200px
| alt =
| IUPAC_name = (1R,3R)-1-(3-((2-(3-(trifluoromethyl)phenyl)thiazol-4-yl)methyl)phenyl)-3-aminocyclopentane-1-carboxylic acid
| CAS_number = 123456-78-9
| ATC_prefix = H05
| ATC_suffix = BX04
}}


== Mechanism of Action ==
'''Upacicalcet''' is a [[calcimimetic]] drug used primarily in the management of [[secondary hyperparathyroidism]] in patients undergoing [[dialysis]] for [[chronic kidney disease]].


Upacicalcet works by binding to and activating the [[calcium-sensing receptor]] (CaSR) on the parathyroid gland. This receptor is responsible for detecting the level of calcium in the blood. When activated by upacicalcet, the CaSR signals the parathyroid gland to reduce the production and release of [[parathyroid hormone]] (PTH), which in turn helps to lower blood calcium levels.
==Mechanism of Action==
Upacicalcet functions as a calcimimetic agent, which means it mimics the action of [[calcium]] on tissues. It acts by binding to the [[calcium-sensing receptor]] (CaSR) on the surface of the [[parathyroid gland]] cells. This binding increases the sensitivity of the receptor to extracellular calcium, thereby reducing the secretion of [[parathyroid hormone]] (PTH). Lower levels of PTH help to manage the mineral and bone disorder associated with chronic kidney disease.


== Clinical Trials ==
==Clinical Use==
Upacicalcet is indicated for the treatment of secondary hyperparathyroidism in patients with chronic kidney disease on dialysis. It is administered intravenously, typically during dialysis sessions. The dosage is adjusted based on the patient's response and serum calcium levels.


Several [[clinical trial]]s have been conducted to assess the safety and efficacy of upacicalcet. These trials have shown promising results, with upacicalcet demonstrating a significant reduction in PTH and serum calcium levels in patients with secondary hyperparathyroidism due to CKD.
==Side Effects==
Common side effects of upacicalcet include [[nausea]], [[vomiting]], and [[hypocalcemia]]. Hypocalcemia, or low blood calcium levels, is a significant concern and requires monitoring. Patients may also experience muscle spasms or tingling sensations due to low calcium levels.


== Potential Benefits ==
==Pharmacokinetics==
Upacicalcet is administered intravenously, allowing for direct entry into the bloodstream. It is metabolized in the liver and excreted primarily through the kidneys. The pharmacokinetic profile supports its use during dialysis sessions, as it can be effectively cleared from the body.


Upacicalcet may offer several potential benefits over existing treatments for hyperparathyroidism and hypercalcemia. These include a more targeted mechanism of action, the potential for fewer side effects, and the possibility of improved patient compliance due to its oral administration.
==Regulatory Status==
Upacicalcet has been approved for use in several countries for the treatment of secondary hyperparathyroidism in dialysis patients. Its approval is based on clinical trials demonstrating its efficacy in reducing PTH levels and managing associated symptoms.


== Side Effects ==
==Related Pages==
* [[Calcimimetic]]
* [[Secondary hyperparathyroidism]]
* [[Chronic kidney disease]]
* [[Dialysis]]


As with any medication, upacicalcet may cause side effects. These can include [[nausea]], [[vomiting]], [[diarrhea]], and [[hypocalcemia]] (low calcium levels). However, these side effects are generally mild and manageable.
[[Category:Calcimimetics]]
 
[[Category:Drugs used in nephrology]]
== Future Directions ==
 
Further research is needed to fully understand the potential benefits and risks of upacicalcet. This includes additional clinical trials and long-term studies to assess the drug's safety and efficacy over time.
 
[[Category:Pharmaceutical Drugs]]
[[Category:Endocrinology]]
[[Category:Nephrology]]
 
{{medicine-stub}}

Revision as of 11:54, 9 February 2025

A calcimimetic drug used in the treatment of secondary hyperparathyroidism


Upacicalcet
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number 123456-78-9
PubChem
DrugBank
ChemSpider
KEGG


Upacicalcet is a calcimimetic drug used primarily in the management of secondary hyperparathyroidism in patients undergoing dialysis for chronic kidney disease.

Mechanism of Action

Upacicalcet functions as a calcimimetic agent, which means it mimics the action of calcium on tissues. It acts by binding to the calcium-sensing receptor (CaSR) on the surface of the parathyroid gland cells. This binding increases the sensitivity of the receptor to extracellular calcium, thereby reducing the secretion of parathyroid hormone (PTH). Lower levels of PTH help to manage the mineral and bone disorder associated with chronic kidney disease.

Clinical Use

Upacicalcet is indicated for the treatment of secondary hyperparathyroidism in patients with chronic kidney disease on dialysis. It is administered intravenously, typically during dialysis sessions. The dosage is adjusted based on the patient's response and serum calcium levels.

Side Effects

Common side effects of upacicalcet include nausea, vomiting, and hypocalcemia. Hypocalcemia, or low blood calcium levels, is a significant concern and requires monitoring. Patients may also experience muscle spasms or tingling sensations due to low calcium levels.

Pharmacokinetics

Upacicalcet is administered intravenously, allowing for direct entry into the bloodstream. It is metabolized in the liver and excreted primarily through the kidneys. The pharmacokinetic profile supports its use during dialysis sessions, as it can be effectively cleared from the body.

Regulatory Status

Upacicalcet has been approved for use in several countries for the treatment of secondary hyperparathyroidism in dialysis patients. Its approval is based on clinical trials demonstrating its efficacy in reducing PTH levels and managing associated symptoms.

Related Pages