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Sensipar
Overview
What is Sensipar?
Sensipar (cinacalcet) is a calcimimetic agent that increases the sensitivity of the calcium-sensing receptor to activation by extracellular calcium. Its empirical formula is CHFN•HCl with a molecular weight of 393.9 g/mol (hydrochloride salt) and 357.4 g/mol (free base). It has one chiral center having an R-absolute configuration. The R-enantiomer is the more potent enantiomer and has been shown to be responsible for pharmacodynamic activity.
Cinacalcet is a white to off-white, crystalline solid that is soluble in methanol or 95% ethanol and slightly soluble in water.
Sensipar tablets are formulated as light-green, film-coated, oval-shaped tablets for oral administration in strengths of 30 mg, 60 mg, and 90 mg of cinacalcet as the free base equivalent (33 mg, 66 mg, and 99 mg as the hydrochloride salt, respectively).
Cinacalcet is described chemically as N-[1-(R)-(-)-(1-naphthyl)ethyl]-3-[3-(trifluoromethyl)phenyl]-1-aminopropane hydrochloride and has the following structural formula:
Inactive Ingredients:
What does Sensipar look like?
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What are the available doses of Sensipar?
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What should I talk to my health care provider before I take Sensipar?
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How should I use Sensipar?
Sensipar is indicated for the treatment of secondary hyperparathyroidism in patients with Chronic Kidney Disease on dialysis.
Sensipar is indicated for the treatment of hypercalcemia in patients with parathyroid carcinoma.
Sensipar tablets should be taken whole and should not be divided. Sensipar should be taken with food or shortly after a meal.
Dosage must be individualized.
What interacts with Sensipar?
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What are the warnings of Sensipar?
Seizures
In three clinical studies of CKD patients on dialysis, 5% of the patients in both the Sensipar and placebo groups reported a history of seizure disorder at baseline. During the trials, seizures (primarily generalized or tonic-clonic) were observed in 1.4% (9/656) of Sensipar-treated patients and 0.4% (2/470) of placebo-treated patients. Five of the nine Sensipar-treated patients had a history of a seizure disorder and two were receiving anti-seizure medication at the time of their seizure. Both placebo-treated patients had a history of seizure disorder and were receiving anti-seizure medication at the time of their seizure. While the basis for the reported difference in seizure rate is not clear, the threshold for seizures is lowered by significant reductions in serum calcium levels. Therefore, serum calcium levels should be closely monitored in patients receiving Sensipar, particularly in patients with a history of a seizure disorder (see PRECAUTIONS, ).
Hypotension and/or Worsening Heart Failure
In postmarketing safety surveillance, isolated, idiosyncratic cases of hypotension, worsening heart failure, and/or arrhythmia have been reported in patients with impaired cardiac function, in which a causal relationship to Sensipar could not be completely excluded and which may be mediated by reductions in serum calcium levels. Clinical trial data showed hypotension occurred in 7% of Sensipar-treated patients and 12% of placebo-treated patients, heart failure occurred in 2% of both Sensipar- and placebo-treated patients.
What are the precautions of Sensipar?
General
Hypocalcemia
Sensipar lowers serum calcium, and therefore patients should be carefully monitored for the occurrence of hypocalcemia. Potential manifestations of hypocalcemia include paresthesias, myalgias, cramping, tetany, and convulsions.
Sensipar treatment should not be initiated if serum calcium is less than the lower limit of the normal range (8.4 mg/dL). Serum calcium should be measured within 1 week after initiation or dose adjustment of Sensipar. Once the maintenance dose has been established, serum calcium should be measured approximately monthly (see ).
If serum calcium falls below 8.4 mg/dL but remains above 7.5 mg/dL, or if symptoms of hypocalcemia occur, calcium-containing phosphate binders and/or vitamin D sterols can be used to raise serum calcium. If serum calcium falls below 7.5 mg/dL, or if symptoms of hypocalcemia persist and the dose of vitamin D cannot be increased, withhold administration of Sensipar until serum calcium levels reach 8.0 mg/dL, and/or symptoms of hypocalcemia have resolved. Treatment should be re-initiated using the next lowest dose of Sensipar (see ).
In the 26-week studies of patients with CKD on dialysis, 66% of patients receiving Sensipar compared with 25% of patients receiving placebo developed at least one serum calcium value < 8.4 mg/dL. Less than 1% of patients in each group permanently discontinued study drug due to hypocalcemia.
Sensipar is not indicated for CKD patients not on dialysis. In CKD patients with secondary HPT not on dialysis, the long-term safety and efficacy of Sensipar have not been established. Clinical studies indicate that Sensipar-treated CKD patients not on dialysis have an increased risk for hypocalcemia compared to Sensipar-treated CKD patients on dialysis, which may be due to lower baseline calcium levels. In a phase 3 study of 32 weeks duration and including 404 subjects (302 cinacalcet, 102 placebo), in which the median dose for cinacalcet was 60 mg at the completion of the study, 80% of Sensipar-treated patients experienced at least one serum calcium value < 8.4 mg/dL compared to 5% of patients receiving placebo.
Adynamic Bone Disease
Adynamic bone disease may develop if iPTH levels are suppressed below 100 pg/mL. One clinical study evaluated bone histomorphometry in patients treated with Sensipar for one year. Three patients with mild hyperparathyroid bone disease at the beginning of the study developed adynamic bone disease during treatment with Sensipar. Two of these patients had iPTH levels below 100 pg/mL at multiple time points during the study. In the three 6-month, phase 3 studies conducted in CKD patients on dialysis, 11% of patients treated with Sensipar had mean iPTH values below 100 pg/mL during the efficacy-assessment phase. If iPTH levels decrease below the NKF-K/DOQI recommended target range (150-300 pg/mL) in patients treated with Sensipar, the dose of Sensipar and/or vitamin D sterols should be reduced or therapy discontinued.
Hepatic Insufficiency
Cinacalcet exposure as assessed by AUC in patients with moderate and severe hepatic impairment (as indicated by the Child-Pugh method) were 2.4 and 4.2 times higher, respectively, than that in normals. Patients with moderate and severe hepatic impairment should be monitored throughout treatment with Sensipar (see , and ).
Information for Patients
It is recommended that Sensipar be taken with food or shortly after a meal. Tablets should be taken whole and should not be divided.
Laboratory Tests
Patients with CKD on Dialysis with Secondary Hyperparathyroidism
Serum calcium and serum phosphorus should be measured within 1 week and iPTH should be measured 1 to 4 weeks after initiation or dose adjustment of Sensipar. Once the maintenance dose has been established, serum calcium and serum phosphorus should be measured approximately monthly, and PTH every 1 to 3 months (see ). All iPTH measurements during the Sensipar trials were obtained using the Nichols IRMA.
In patients with end-stage renal disease, testosterone levels are often below the normal range. In a placebo-controlled trial in patients with CKD on dialysis, there were reductions in total and free testosterone in male patients following six months of treatment with Sensipar. Levels of total testosterone decreased by a median of 15.8% in the Sensipar-treated patients and by 0.6% in the placebo-treated patients. Levels of free testosterone decreased by a median of 31.3% in the Sensipar-treated patients and by 16.3% in the placebo-treated patients. The clinical significance of these reductions in serum testosterone is unknown.
Patients with Parathyroid Carcinoma
Serum calcium should be measured within 1 week after initiation or dose adjustment of Sensipar. Once maintenance dose levels have been established, serum calcium should be measured every 2 months (see ).
Drug Interactions and/or Drug/Laboratory Test Interactions
See CLINICAL PHARMACOLOGY, and .
Effect of Sensipar on other drugs:
Drugs metabolized by cytochrome P450 2D6 (CYP2D6): Sensipar is a strong in vitro, as well as in vivo, inhibitor of CYP2D6. Therefore, dose adjustments of concomitant medications that are predominantly metabolized by CYP2D6 (eg, metoprolol and carvedilol) and particularly those with a narrow therapeutic index (eg, flecainide, vinblastine, thioridazine and most tricyclic antidepressants) may be required.
Desipramine: Concurrent administration of cinacalcet (90 mg) with desipramine (50 mg) increased the exposure of desipramine by 3.6 fold in CYP2D6 extensive metabolizers.
Amitriptyline: Concurrent administration of 25 mg or 100 mg cinacalcet with 50 mg amitriptyline increased amitriptyline exposure and nortriptyline (active metabolite) exposure by approximately 20% in CYP2D6 extensive metabolizers.
Midazolam: There were no significant differences in the pharmacokinetics of midazolam, a CYP3A4 and CYP3A5 substrate, in subjects receiving 90 mg cinacalcet once daily for 5 days and a single dose of 2 mg midazolam on day 5 as compared to those of subjects receiving 2 mg midazolam alone. This suggests that cinacalcet would not affect the pharmacokinetics of drugs predominantly metabolized by CYP3A4 and CYP3A5.
Effect of other drugs on Sensipar:
Sensipar is metabolized by multiple cytochrome P450 enzymes, primarily CYP3A4, CYP2D6, and CYP1A2.
Ketoconazole: Sensipar is metabolized in part by CYP3A4. Co-administration of ketoconazole, a strong inhibitor of CYP3A4, increased cinacalcet exposure following a single 90 mg dose of Sensipar by 2.3 fold. Dose adjustment of Sensipar may be required and PTH and serum calcium concentrations should be closely monitored if a patient initiates or discontinues therapy with a strong CYP3A4 inhibitor (e.g., ketoconazole, erythromycin, itraconazole; see ).
Carcinogenesis, Mutagenesis, and Impairment of Fertility
Carcinogenicity:
Mutagenicity:
Impairment of Fertility:
Pregnancy Category C
In pregnant female rats given oral gavage doses of 2, 25, 50 mg/kg/day during gestation no teratogenicity was observed at doses up to 50 mg/kg/day (exposure 4 times those resulting with a human oral dose of 180 mg/day based on AUC comparison). Decreased fetal body weights were observed at all doses (less than 1 to 4 times a human oral dose of 180 mg/day based on AUC comparison) in conjunction with maternal toxicity (decreased food consumption and body weight gain).
In pregnant female rabbits given oral gavage doses of 2, 12, 25 mg/kg/day during gestation no adverse fetal effects were observed (exposures less than with a human oral dose of 180 mg/day based on AUC comparisons). Reductions in maternal food consumption and body weight gain were seen at doses of 12 and 25 mg/kg/day.
In pregnant rats given oral gavage doses of 5, 15, 25 mg/kg/day during gestation through lactation no adverse fetal or pup (post-weaning) effects were observed at 5 mg/kg/day (exposures less than with a human therapeutic dose of 180 mg/day based on AUC comparisons). Higher doses of 15 and 25 mg/kg/day (exposures 2-3 times a human oral dose of 180 mg/day based on AUC comparisons) were accompanied by maternal signs of hypocalcemia (periparturient mortality and early postnatal pup loss), and reductions in postnatal maternal and pup body-weight gain. Sensipar has been shown to cross the placental barrier in rabbits.
There are no adequate and well-controlled studies in pregnant women. Sensipar should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Lactating Women
Studies in rats have shown that Sensipar is excreted in the milk with a high milk-to-plasma ratio. It is not known whether this drug is excreted in human milk. Considering these data in rats and because many drugs are excreted in human milk and because of the potential for clinically significant adverse reactions in infants from Sensipar, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the lactating woman.
Pediatric Use
The safety and efficacy of Sensipar in pediatric patients have not been established.
Geriatric Use
Of the 1136 patients enrolled in the Sensipar phase 3 clinical program, 26% were ≥ 65 years old, and 9% were ≥ 75 years old. No differences in the safety and efficacy of Sensipar were observed in patients greater or less than 65 years of age (see , Geriatric patients ).
What are the side effects of Sensipar?
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What should I look out for while using Sensipar?
Sensipar is contraindicated in patients with hypersensitivity to any component(s) of this product.
What might happen if I take too much Sensipar?
Doses titrated up to 300 mg once daily have been safely administered to patients on dialysis. Overdosage of Sensipar may lead to hypocalcemia. In the event of overdosage, patients should be monitored for signs and symptoms of hypocalcemia and appropriate measures taken to correct serum calcium levels (see ).
Since Sensipar is highly protein bound, hemodialysis is not an effective treatment for overdosage of Sensipar.
How should I store and handle Sensipar?
Store at 20°-25°C (68°-77°F) (see USP Controlled Room Temperature). Protect from light.Dispense in a tight, light-resistant container.Store at 20°-25°C (68°-77°F) (see USP Controlled Room Temperature). Protect from light.Dispense in a tight, light-resistant container.Sensipar 30 mg tablets are formulated as light-green, film-coated, oval-shaped tablets marked with “AMG” on one side and “30” on the opposite side.Sensipar 60 mg tablets are formulated as light-green, film-coated, oval-shaped tablets marked with “AMG” on one side and “60” on the opposite side.Sensipar 90 mg tablets are formulated as light-green, film-coated, oval-shaped tablets marked with “AMG” on one side and “90” on the opposite side.They are supplied by as follows:Sensipar 30 mg tablets are formulated as light-green, film-coated, oval-shaped tablets marked with “AMG” on one side and “30” on the opposite side.Sensipar 60 mg tablets are formulated as light-green, film-coated, oval-shaped tablets marked with “AMG” on one side and “60” on the opposite side.Sensipar 90 mg tablets are formulated as light-green, film-coated, oval-shaped tablets marked with “AMG” on one side and “90” on the opposite side.They are supplied by as follows:Sensipar 30 mg tablets are formulated as light-green, film-coated, oval-shaped tablets marked with “AMG” on one side and “30” on the opposite side.Sensipar 60 mg tablets are formulated as light-green, film-coated, oval-shaped tablets marked with “AMG” on one side and “60” on the opposite side.Sensipar 90 mg tablets are formulated as light-green, film-coated, oval-shaped tablets marked with “AMG” on one side and “90” on the opposite side.They are supplied by as follows:Sensipar 30 mg tablets are formulated as light-green, film-coated, oval-shaped tablets marked with “AMG” on one side and “30” on the opposite side.Sensipar 60 mg tablets are formulated as light-green, film-coated, oval-shaped tablets marked with “AMG” on one side and “60” on the opposite side.Sensipar 90 mg tablets are formulated as light-green, film-coated, oval-shaped tablets marked with “AMG” on one side and “90” on the opposite side.They are supplied by as follows:
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Secondary hyperparathyroidism (HPT) in patients with chronic kidney disease (CKD) is a progressive disease, associated with increases in parathyroid hormone (PTH) levels and derangements in calcium and phosphorus metabolism. Increased PTH stimulates osteoclastic activity resulting in cortical bone resorption and marrow fibrosis. The goals of treatment of secondary hyperparathyroidism are to lower levels of PTH, calcium, and phosphorus in the blood, in order to prevent progressive bone disease and the systemic consequences of disordered mineral metabolism. In CKD patients on dialysis with uncontrolled secondary HPT, reductions in PTH are associated with a favorable impact on bone-specific alkaline phosphatase (BALP), bone turnover and bone fibrosis.
The calcium-sensing receptor on the surface of the chief cell of the parathyroid gland is the principal regulator of PTH secretion. Sensipar directly lowers PTH levels by increasing the sensitivity of the calcium-sensing receptor to extracellular calcium. The reduction in PTH is associated with a concomitant decrease in serum calcium levels.
Non-Clinical Toxicology
Sensipar is contraindicated in patients with hypersensitivity to any component(s) of this product.Drug Interactions
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
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