Crofelemer

Indications

CANALEVIA-CA1 is indicated for the treatment of chemotherapy-induced diarrhea in dogs.

Dosage and Administration

Administer 1 tablet orally twice daily for 3 days for dogs weighing ≤ 140 pounds. Administer 2 tablets orally twice daily for 3 days for dogs weighing >140 pounds. Tablets should not be broken, crushed, or chewed. If the tablet is chewed, one additional dose may be administered. Give with or without food.

Contraindications

Do not use in patients with a known hypersensitivity to crofelemer.

Warnings

Not for use in humans. Keep this and all medications out of reach of children. Consult a physician in case of accidental ingestion by humans. Keep CANALEVIA-CA1 in a secure location out of reach of dogs, cats, and other animals to prevent accidental ingestion or overdose.

Precautions

The safe use of CANALEVIA-CA1 has not been evaluated in dogs that are pregnant, lactating, or intended for breeding. Prior to using CANALEVIA-CA1, rule out infectious etiologies of diarrhea. Prescribing CANALEVIA-CA1 to dogs with diarrhea secondary to infectious etiologies may delay appropriate treatment.

Adverse Reactions

In a masked, randomized study to support a reasonable expectation of effectiveness (CANA-001a) there was similar incidence of adverse events in dogs administered Crofelemer (not commercial formulation) compared to control dogs administered a vehicle control. Crofelemer was administered orally twice a day for three days as enteric-coated beads containing 40 mg of the active ingredient. The vehicle control was enteric-coated beads without the active ingredient. The dogs had daily assessments for changes in attitude, hydration, appetite, and abdominal palpation. Table 1 shows the adverse reactions during CANA-001a study. Table 1. Adverse Reactions in CANA-001a Study to Support Reasonable Expectation of Effectiveness Adverse Reaction 1 Crofelemer N = 29 Vehicle Control N = 32 Appetite decreased 7 (24%) 9 (28%) Attitude depressed 5 (17%) 5 (16%) Activity decreased 4 (14%) 4 (13%) Dehydration 2 4 (14%) 5 (16%) Abdominal palpation indicated pain 3 3 (10%) 5 (16%) Vomiting 1 (3%) 2 (6%) 1 Dogs may have experienced more than one occurrence and more than one type of abnormal assessment during the study 2 Two crofelemer treated dogs and one vehicle control dog were administered fluid therapy 3 One of the vehicle control dogs was reported to not allow abdominal palpation at one timepoint on Day 2 In an open-label pilot study (CANA-001b) 48 dogs were administered crofelemer (not commercial formulation) orally twice a day for three days. The adverse reactions included decreased appetite in 16/48 (33%) dogs, vomiting in 3 (6%) dogs, decreased activity in 3 dogs (6%), abdominal pain in 1 (2%) dog, and 1 (2%) dog had blood in feces. In a separate pilot clinical field study (CANA-003), dogs with acute diarrhea were randomized to receive crofelemer or placebo tablets. The study included 22 dogs administered crofelemer (not commercial formulation) tablets and 112 dogs administered 125 mg CANALEVIA-CA1 tablets. There were 66 dogs who received placebo tablets. Dogs were administered tablets orally twice a day for three days. Hematology and clinical chemistry were obtained prior to dosing and on Day 3 at the end of the study. Table 2 shows adverse reactions during the study. Table 2. Adverse Reactions in Pilot Field Study CANA-003 Adverse Reaction Crofelemer N=134 Placebo N=66 Vomiting 11 (8%) 1 (2%) Decreased blood glucose 1 10 (8%) 3 (5%) Urinary system abnormality 2 10 (8%) 2 (3%) Upper respiratory signs 3 7 (5%) 0 (0%) Decreased blood calcium 4 5 (4%) 0 (0%) 1 Dogs with decreased blood glucose at study end had normal blood glucose (reference range 74-145 mg/dL) prior to dosing. None of the dogs were reported to be clinically affected by the decreased blood glucose. The low blood glucose values ranged from 34 to 71 mg/dL. 2 Urinary system abnormalities were documented as development of a urinary tract infection, cystitis, or a worsening pyuria in the urine. 3 Upper respiratory signs included coughing, nasal discharge, sneezing, and congestion. 4 Dogs with decreased serum calcium (reference range 8.7-12 mg/dL) at study end had normal calcium at screening. The decreased calcium values were not associated with decreased albumin values. None of the dogs were reported to be clinically affected by the decreased serum calcium. The lowest reported calcium was 5.8 mg/dL. Five dogs administered crofelemer and one placebo group dog were removed from the study for no improvement in stools. One additional dog administered crofelemer was removed for hemorrhagic stool. CONTACT INFORMATION: To report suspected adverse drug events and/or to obtain a copy of the Safety Data Sheet (SDS) or for technical assistance, call Jaguar Animal Health at 1-877-787-3001. For additional information about adverse drug experience reporting for animal drugs, contact FDA at 1-888-FDA-VETS or http://www.fda.gov/reportanimalae.

Description

CANALEVIA-CA1 (crofelemer delayed-release tablets) is an antidiarrheal, enteric-coated drug product for oral administration. CANALEVIA-CA1 containing 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. Chemical Structure Image

Storage

Store at 20°C-25°C (68°F-77°F) with excursions permitted between 15°C-30°C (59°F-86°F).

FDA adverse event reports

The FDA Center for Veterinary Medicine publishes the adverse event reports it receives through openFDA. The counts below are the reports naming crofelemer as an active ingredient for each species this label names, as returned on 2026-09-16, coded by the VeDDRA reaction term the reporter chose. Reactions are counted per report, so one report can appear under several terms.

These are counts, not rates. Reporting is voluntary, the number of animals treated is not known, and a widely used product accumulates reports for that reason alone. A report records that an event followed a dose; it does not establish that the product caused it. The counts say nothing about how one product compares with another.