Tenapanor(LuciTena)

Tenapanor (LuciTena) is a sodium/hydrogen exchanger 3 (NHE3) inhibitor that can be used as monotherapy or in combination with phosphate binders.

Lucius Related Certificates

Drug Test Report

Drug Approval Certificate

Dosage and Administration of Tenapanor (LuciTena)

1. Patient Monitoring

Serum phosphorus levels should be monitored, and the dose should be adjusted as needed to manage gastrointestinal tolerability. The goals of dose adjustment encompass both serum phosphorus control and gastrointestinal tolerability.

2. Method of Administration

Tenapanor (LuciTena) should be taken immediately before the first meal (breakfast) and the last meal (dinner) of the day.

Tenapanor (LuciTena) should not be taken immediately before hemodialysis treatment; instead, it should be taken immediately before the next meal after dialysis, because diarrhea may occur after patients take Tenapanor (LuciTena).

The dosing schedule is based on the finding that taking Tenapanor (LuciTena) 5 to 10 minutes before a meal increases 24-hour fecal phosphorus excretion compared with taking it after a meal or on an empty stomach. Therefore, Tenapanor (LuciTena) should be tied to meal times and should not be taken on an empty stomach or after a meal.

3. Recommended Dosage

The recommended dosage is 30 mg orally twice daily, taken before the morning and evening meals.

Tenapanor (LuciTena) can be used as monotherapy or in combination with phosphate binders.

4. Missed Dose

If a dose is missed, the missed dose should be skipped, and the next dose should be taken at the regular time before the next meal. Do not take two doses at the same time.

Dosage Adjustments

Dose Adjustment for Toxicity

Tenapanor (LuciTena) should be discontinued in patients with severe diarrhea. For mild to moderate diarrhea, events mostly resolve over time or with dose reduction; dose reduction may be considered.

Dose Adjustment in Special Populations

Geriatric patients, patients with hepatic impairment, and patients with renal impairment: no specific dosage recommendations.

Use in Specific Populations of Tenapanor (LuciTena)

1. Pregnancy

Tenapanor (LuciTena) is minimally absorbed systemically, with plasma concentrations below the lower limit of quantification (<0.5 ng="">

2. Lactation

Tenapanor (LuciTena) and its major metabolite M1 were not detected in the breast milk of lactating women.

Consider the benefits of breastfeeding for infant development and health, the mother's clinical need for Tenapanor (LuciTena), and any potential adverse effects of Tenapanor (LuciTena) or the mother's underlying disease on the breastfed infant.

3. Pediatric Use

Tenapanor (LuciTena) is contraindicated in patients under 6 years of age.

4. Geriatric Use

Clinical studies of Tenapanor (LuciTena) did not include a sufficient number of patients aged 65 years and older to determine whether they respond differently from younger patients.

5. Hepatic Impairment

In subjects with normal hepatic function and moderate hepatic impairment, Tenapanor (LuciTena) showed minimal systemic bioavailability, with plasma concentrations below the lower limit of quantification (<0.5 ng="">

6. Renal Impairment

In CKD patients receiving dialysis (estimated glomerular filtration rate [eGFR] below 15 mL/min/1.73 m²), steady-state plasma concentrations of M1 were not significantly different from those in healthy subjects receiving similar doses of Tenapanor (LuciTena).

Contraindications of Tenapanor (LuciTena)

Tenapanor (LuciTena) is contraindicated in pediatric patients under 6 years of age due to the risk of diarrhea and severe dehydration.

Tenapanor (LuciTena) is contraindicated in patients with known or suspected mechanical gastrointestinal obstruction.

Warnings and Precautions for Tenapanor (LuciTena)

Diarrhea

Tenapanor (LuciTena) acts locally in the intestine, and amplification of its pharmacologic effect can lead to gastrointestinal adverse reactions; diarrhea is the most common adverse reaction in patients treated with Tenapanor (LuciTena). If diarrhea is severe or prolonged, there is a risk of dehydration.

Monitor patients for the occurrence and severity of diarrhea, and assess volume status and electrolytes when diarrhea occurs; Tenapanor (LuciTena) should be discontinued in patients with severe diarrhea, and patients should be instructed to contact their healthcare provider. For mild to moderate diarrhea, dose reduction may be considered with continued observation. Tenapanor (LuciTena) should not be used with stool softeners or laxatives.

Adverse Reactions of Tenapanor (LuciTena)

Most common adverse reaction: diarrhea.

Drug Interactions of Tenapanor (LuciTena)

Organic Anion Transporting Polypeptide 2B1 (OATP2B1) Substrates

Tenapanor (LuciTena) is an inhibitor of the intestinal uptake transporter OATP2B1. Exposure to drugs that are OATP2B1 substrates may be decreased when coadministered with Tenapanor (LuciTena). Monitor for signs of loss of efficacy and adjust the dose of the concomitant drug as needed.

Other Transporters

Tenapanor (LuciTena) inhibits OATP2B1 but is not an inhibitor of P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), OATP1B1, OATP1B3, or PEPT1. M1 does not inhibit P-gp, BCRP, OATP1B1, OATP1B3, OAT1, OAT3, OCT2, MATE1, or MATE2-K. Tenapanor (LuciTena) is not a substrate of P-gp, BCRP, OATP1B1, or OATP1B3; M1 is a substrate of P-gp.

Interactions Mediated by Cytochrome P450 (CYP) Metabolism

Tenapanor (LuciTena) and M1 do not inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, or CYP2D6 in vitro, and do not induce CYP1A2 or CYP2B6 in vitro. Tenapanor (LuciTena) is primarily metabolized by CYP3A4/5.

CYP3A4 inhibitors: After a single dose of Tenapanor (LuciTena) was coadministered with repeated doses of the CYP3A4 inhibitor itraconazole, the mean AUC and Cmax of M1 decreased in healthy subjects; after coadministration with itraconazole, plasma concentrations of Tenapanor (LuciTena) were mostly below the lower limit of quantification (<0.5 ng="">

Interactions with Phosphate Binders

In vitro studies suggest that Tenapanor (LuciTena) may bind to sevelamer carbonate, but did not suggest that it may bind to calcium carbonate or calcium acetate.

Sodium Polystyrene Sulfonate (SPS)

Tenapanor (LuciTena) and sodium polystyrene sulfonate should be administered at least 3 hours apart. SPS can bind to many commonly used oral medications.