Crofelemer
FDA Drug Information • Also known as: Mytesi
- Brand Names
- Mytesi
- Drug Class
- Antidiarrheal [EPC]
- Route
- ORAL
- Dosage Form
- TABLET, COATED
- Product Type
- HUMAN PRESCRIPTION DRUG
Description
11 DESCRIPTION MYTESI (crofelemer) delayed-release tablets is an anti-diarrheal, enteric-coated drug product for oral administration. It contains 125 mg of crofelemer, a botanical drug substance that is derived from the red latex of Croton lechleri Müll. Arg. Crofelemer is an oligomeric proanthocyanidin mixture primarily composed of (+)–catechin, (–)–epicatechin, (+)–gallocatechin, and (–)–epigallocatechin monomer units linked in random sequence, as represented below. The average degree of polymerization for the oligomers ranges between 5 and 7.5, as determined by phloroglucinol degradation. R = H or OH range n = 3 to 5.5 Inactive ingredients: colloidal silicon dioxide, croscarmellose sodium, magnesium stearate, and microcrystalline cellulose. Coating ingredients: ethylacrylate and methylacrylate copolymer dispersion, talc, triethyl citrate, and white dispersion which contains xanthan gum, titanium dioxide, propyl paraben, and methyl paraben. The following chemical structure for MYTESI (crofelemer) is delayed-release tablets is an anti-diarrheal, enteric-coated drug product for oral administration. It contains 125 mg of crofelemer, a botanical drug substance that is derived from the red latex of Croton lechleri Müll. Arg. Crofelemer is an oligomeric proanthocyanidin mixture primarily composed of (+)–catechin, (–)–epicatechin, (+)–gallocatechin, and (–)–epigallocatechin monomer units linked in random sequence, as represented below. The average degree of polymerization for the oligomers ranges between 5 and 7.5, as determined by phloroglucinol degradation.
What Is Crofelemer Used For?
1 INDICATIONS AND USAGE MYTESI is indicated for symptomatic relief of non-infectious diarrhea in adult patients with HIV/AIDS on anti-retroviral therapy. MYTESI is an anti-diarrheal indicated for the symptomatic relief of non-infectious diarrhea in adult patients with HIV/AIDS on anti-retroviral therapy. ( 1 )
Dosage and Administration
2 DOSAGE AND ADMINISTRATION Before starting MYTESI, rule out infectious etiologies of diarrhea [see Warnings and Precautions ( 5.1 )] . The recommended adult dosage of MYTESI is 125 mg taken orally two times a day, with or without food. Do not crush or chew MYTESI tablets. Swallow whole. Before starting MYTESI, rule out infectious etiologies of diarrhea. ( 2 , 5.1 ) The recommended adult dosage is 125 mg taken orally twice a day, with or without food. ( 2 ) Do not crush or chew the tablets. Swallow whole. ( 2 )
Side Effects (Adverse Reactions)
6 ADVERSE REACTIONS Most common adverse reactions (≥ 3%) are upper respiratory tract infection, bronchitis, cough, flatulence and increased bilirubin. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Napo Pharmaceuticals at 1-844-722-8256 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. A total of 696 HIV-positive patients in three placebo-controlled trials received MYTESI for a mean duration of 78 days. Of the total population across the three trials, 229 patients received a dosage of 125 mg twice a day for a mean duration of 141 days, and 171 patients received one of four higher than recommended dosages for a mean duration of 139 days (N=69) 14 days (N=102), 146 days (N=54), and 14 days (N=242), respectively. Adverse reactions in patients treated with MYTESI 125 mg twice daily that occurred in at least 2% of patients and at a higher incidence than placebo are provided in Table 1 . Table 1: Common Adverse Reactions occurring in at least 2% of patients and at a higher incidence than placebo in HIV-Positive Patients in Three Placebo-Controlled Trials Adverse Reaction MYTESI 125 mg Twice Daily N = 229 n (%) Placebo N = 274 n (%) Upper respiratory tract infection 13 (6) 4 (2) Bronchitis 9 (4) 0 Cough 8 (4) 3 (1) Flatulence 7 (3) 3 (1) Increased bilirubin 7 (3) 3 (1) Nausea 6 (3) 4 (2) Back pain 6 (3) 4 (2) Arthralgia 6 (3) 0 Urinary tract infection 5 (2) 2 (1) Nasopharyngitis 5 (2) 2 (1) Musculoskeletal pain 5 (2) 1 (<1) Hemorrhoids 5 (2) 0 Giardiasis 5 (2) 0 Anxiety 5 (2) 1 (<1) Increased alanine aminotransferase 5 (2) 3 (1) Abdominal distension 5 (2) 1 (<) Less common adverse reactions that occurred in between 1% and 2% of patients taking 125 mg twice daily of MYTESI were abdominal pain, acne, increased aspartate aminotransferase, increased conjugated bilirubin, increased unconjugated blood bilirubin, constipation, depression, dermatitis, dizziness, dry mouth, dyspepsia, gastroenteritis, herpes zoster, nephrolithiasis, pain in extremity, pollakiuria, sinusitis and decreased white blood cell count.
Drug Interactions
7 DRUG INTERACTIONS 7.1 Nelfinavir, Zidovudine, and Lamivudine MYTESI administration did not have a clinically relevant interaction with nelfinavir, zidovudine, or lamivudine in a drug-drug interaction trial [see Clinical Pharmacology ( 12.3 )] .
Contraindications
4 CONTRAINDICATIONS None. None ( 4 )
Pregnancy and Breastfeeding
8.1 Pregnancy Risk Summary Crofelemer is minimally absorbed systemically by the oral route of administration and maternal use is not expected to result in fetal exposure to the drug [see Clinical Pharmacology ( 12.3 )] . In pregnant rats, no adverse fetal effects were observed with oral administration of crofelemer at doses up to 177 times the recommended clinical dose during the period of organogenesis. In pregnant rabbits, an increase in fetal resorptions and abortions compared to controls were observed with crofelemer at a dose of 96 times the recommended clinical dose. However, it is not clear whether these effects in rabbits are related to the maternal toxicity (decreased body weight and decreased food consumption) observed at this dose (see Data) . The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data Crofelemer was not teratogenic and did not produce embryofetal toxicity in pregnant rats following oral administration at doses up to 738 mg/kg/day during the period of organogenesis. The 738 mg/kg/day dose is 177 times the recommended daily human dose of 4.2 mg/kg/day. Crofelemer was not teratogenic in pregnant rabbits following oral administration at doses up to 400 mg/kg/day during the period of organogenesis. At a dose level of 400 mg/kg/day, which is 96 times the recommended daily human dose of 4.2 mg/kg/day, crofelemer produced an increase in fetal resorptions and abortions compared to controls. However, it is not clear whether these effects are related to the maternal toxicity (decreased body weight and decreased food consumption) observed.
How Supplied
16 HOW SUPPLIED /STORAGE AND HANDLING MYTESI (crofelemer) 125 mg delayed-release tablets are white, oval tablets printed on one side with 125SLXP. They are available in the following package size: Bottles of 60: NDC 70564-802-60 Store at 20°C-25°C (68°F-77°F); excursions permitted between 15°C-30°C (59°F-86°F). See USP Controlled Room Temperature.
About This Information
This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.
What are side effects?
Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.
What are drug interactions?
Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.