Chenodiol (Monograph)

Brand names: Chenodal, Ctexli™
Drug class: Cholelitholytic Agents

Medically reviewed by Drugs.com on Aug 10, 2025. Written by ASHP.

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Introduction

Naturally occurring human bile acid.^{1 24}

Uses for Chenodiol

Gallstone Dissolution

Used for dissolution of gallstones in patients with radiolucent stones in well-opacifying gallbladders who are not candidates for elective surgery because of systemic disease or advanced age (Chenodal only; designated an orphan drug by FDA for this use).^{1 3}

For symptomatic patients who are surgical candidates, laparoscopic cholecystectomy is recommended; for patients who are not surgical candidates, oral dissolution therapy (e.g., ursodeoxycholic acid or chenodiol) or extracorporeal shock wave therapy may be considered.^{22 23}

Cerebrotendinous Xanthomatosis (CTX)

Used for the treatment of CTX in adults (Ctexli™ only; designated an orphan drug by FDA for this use).^{3 24}

CTX is a rare, genetic lipid storage disorder, manifesting as a deficiency in bile acids and subsequent accumulation of cholesterol metabolites in various tissues, including the brain and tendons.²⁶ Treatment with chenodiol is aimed at preventing complications of CTX.²⁶

Chenodiol Dosage and Administration

General

Pretreatment Screening

• Screen patients treated for gallstone dissolution with chenodiol carefully to evaluate risks and benefits of treatment.¹ Considerations for treatment include size and opacity of gallstones, gallbladder visualization, candidacy for surgery, and need for long-term use of chenodiol.¹

• Screen for pre-existing hepatic dysfunction.¹ Obtain baseline ALT, AST, and total bilirubin levels.^{1 24}

• For patients receiving treatment for gallstone dissolution, screen for bile duct abnormalities.¹

• For patients receiving treatment for gallstone dissolution, obtain pregnancy status.¹

Patient Monitoring

• For patients receiving treatment for gallstone dissolution, monitor for pregnancy in female patients.¹

• For patients receiving treatment for gallstone dissolution, monitor serum aminotransferase levels monthly for the first 3 months and then every 3 months thereafter.¹

• For patients receiving treatment for cerebrotendinous xanthomatosis, monitor serum aminotransferase and total bilirubin levels yearly and as clinically indicated.²⁴

• For patients receiving treatment for gallstone dissolution, monitor serum cholesterol every 6 months.¹

• For patients receiving treatment for gallstone dissolution, monitor WBC count.¹

• For patients receiving treatment for gallstone dissolution, monitor for dissolution every 6–9 months with either oral cholecystograms or ultrasonograms.¹

Administration

Oral Administration

Administer orally 2-3 times daily; swallow whole.^{1 24}

For Ctexli^TM, if dose missed, advise patient to skip missed dose and resume taking prescribed dose at next scheduled time.²⁴

Dosage

Adults

Gallstone Dissolution (Chenodal)

Oral

Recommended dosage range is 13–16 mg/kg daily, given in 2 divided doses.¹ Recommended initial dosage is 250 mg twice daily for the first 2 weeks.¹ Increase dosage by 250 mg daily each week thereafter, until the recommended or maximum tolerated dosage is reached.¹ Discontinue if no response by 18 months.¹

Dosages <10 mg/kg daily usually are ineffective and may be associated with increased risk of cholecystectomy; such dosages are not recommended.¹ More information on recommended adult dosages is presented in Table 1.

Cerebrotendinous Xanthomatosis (Ctexli™)

Oral

Recommended dosage is 250 mg three times daily with or without food.²⁴

Dosage Modifications for Toxicity

Diarrhea

In patients with gallstones, if diarrhea occurs, temporarily adjust dosage until symptoms abate, after which the previous dosage usually is tolerated.¹

Elevated Aminotransferase Levels

In patients with gallstones, if aminotransferase levels are elevated >3 times ULN, discontinue chenodiol treatment.¹

In patients with cerebrotendinous xanthomatosis, if liver transaminase (ALT, AST) levels are elevated >3 times ULN or total bilirubin level is >2 times ULN, interrupt treatment until the levels have returned to baseline values.²⁴ Monitor liver transaminase and total bilirubin levels yearly and as clinically indicated.²⁴

Special Populations

Hepatic Impairment

For patients receiving treatment with Chenodal for gallstone dissolution, use is contraindicated.¹ No specific dosage recommendations at this time for Ctexli™.²⁴

Renal Impairment

No specific dosage recommendations at this time.^{1 24}

Geriatric Patients

No specific dosage recommendations at this time.^{1 24}

Cautions for Chenodiol

Contraindications

Chenodal

• Women who are or may become pregnant.¹

• Presence of known hepatocyte dysfunction or bile duct abnormalities (e.g., intrahepatic cholestasis, primary biliary cirrhosis, sclerosing cholangitis).¹

• Gallbladder confirmed as nonvisualizing after 2 consecutive single doses of dye, radiopaque stone, gallstone complications, or compelling reasons for gallbladder surgery (e.g., unremitting acute cholecystitis, cholangitis, biliary obstruction, gallstone pancreatitis, biliary-GI fistula).¹

Ctexli™

• None.²⁴

Warnings/Precautions

Hepatotoxicity

Chenodal

Significant hepatotoxicity reported in clinical trials.¹

Serum aminotransferase (mainly ALT) concentrations increased to >3 times ULN, recurred on rechallenge with the drug, and required drug discontinuance in 2–3% of patients receiving chenodiol.¹ Concentrations returned to normal following drug withdrawal.¹

Reserve chenodiol for carefully selected patients without preexisting liver disease carefully monitor serum aminotransferase concentrations to detect drug-induced liver toxicity.¹ Discontinue if aminotransferase levels are elevated >3 times ULN.¹

Ctexli™

Obtain baseline liver transaminase and total bilirubin levels; interrupt treatment and allow levels to normalize.²⁴ If elevated levels persist or recur, consider treatment discontinuation.²⁴

Risk of Colon Cancer

Chenodal

Bile acids might contribute to human colon cancer, but direct evidence is lacking.¹

Bile acids, including chenodiol and lithocholic acid, have no carcinogenic potential in animal models, but have been shown to increase the number of tumors when administered with certain carcinogens.¹

The possibility that chenodiol therapy might contribute to colon cancer in otherwise susceptible individuals cannot be ruled out.¹

Specific Populations

Pregnancy

Chenodal: may cause fetal harm based on animal studies.¹ No human pregnancy/ fetal data available.¹ Chenodal is contraindicated in women who are or may become pregnant.¹

Ctexli™: findings of increased risk from animal studies have not been observed with human use.²⁴

Lactation

Not known whether chenodiol is distributed into human milk.^{1 24} Use with caution.^{1 24}

Pediatric Use

Safety and efficacy not established.^{1 24}

Geriatric Use

Not evaluated in patients 65 years and older.²⁴

Hepatic Impairment

Chenodiol is hepatically metabolized.^{1 24} Chenodal is contraindicated for gallstone dissolution in patients with hepatic impairment.¹ No manufacturer recommendation on use of Ctexli™ for cerebrotendinous xanthomatosis in patients with pre-existing hepatic impairment.²⁴

Renal Impairment

No information on use in patients with renal impairment.^{1 24}

Common Adverse Effects

Chenodal: Serum aminotransferase elevations, diarrhea (usually mild, translucent, well tolerated), increased serum total cholesterol and low-density lipoprotein (LDL)-cholesterol, and decreased leukocyte count (not below 3000/mm³) have been reported.¹

Ctexli™: The most common adverse reactions (incidence >14%) are diarrhea, headache, abdominal pain, constipation, hypertension, muscular weakness, upper respiratory infection.²⁴

Drug Interactions

Chenodiol and its glyco- and tauro-conjugates not expected to inhibit CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, or 3A4, or induce CYP1A2 or 2B6.²⁴ Chenodiol and its tauro-conjugate may upregulate CYP3A4 mRNA (clinical significance unknown).²⁴

Glyco- and tauro-conjugates of chenodiol are high affinity substrates for bile salt export pump (BSEP); chenodiol may also inhibit organic anion transporting polypeptide (OATP)1B1 and 1B3 (clinical significance unknown).²⁴

Chenodiol and its glyco- and tauro-conjugates not predicted to inhibit P-glycoprotein, breast cancer resistance protein (BCRP), OATP2B1, organic anion transporter (OAT)1, OAT3, organic cation transporter (OCT)1, OCT2, multidrug and toxin compound extrusion (MATE)1, or MATE2-K.²⁴

Specific Drugs

Chenodiol Pharmacokinetics

Absorption

Bioavailability

Following oral administration, well absorbed from the small intestine.^{1 24} Undergoes enterohepatic circulation.^{1 24}

In patients with cerebrotendinous xanthomatosis, median time to maximum concentration following oral administration was 3 hours.²⁴

Distribution

Extent

After the drug is conjugated in the liver, it is distributed into bile.^{1 24}

Not known whether chenodiol is distributed into human milk.^{1 24}

Plasma Protein Binding

Approximately 98%.²⁴

Elimination

Metabolism

Chenodiol is conjugated with glycine and taurine in the liver.^{1 24}

Elimination Route

Chenodiol is converted by bacterial action in the colon to lithocholic acid.^{1 24} About 80% of litholate is excreted in the feces; the remainder is absorbed and converted in the liver to poorly absorbed sulfolithocholyl conjugates.^{1 24} During chenodiol therapy there is only a minor increase in biliary lithocholate, while fecal bile acids are increased 3- to 4-fold.^{1 24}

Stability

Storage

Oral

Tablets

Tightly closed containers at 20–25°C.^{1 24}

For Ctexli™ tablets, excursions permitted between 15–30°C.²⁴

Actions

• Suppresses hepatic synthesis of both cholesterol and cholic acid, gradually replacing the latter and its metabolite, deoxycholic acid, in an expanded bile acid pool.¹

• These actions contribute to biliary cholesterol desaturation and gradual dissolution of radiolucent cholesterol gallstones in the presence of a gallbladder visualized by oral cholecystography.¹

• Has no effect on radiopaque (calcified) gallstones or radiolucent bile pigment stones.¹

• In cerebrotendinous xanthomatosis (CTX), major bile acid synthesis pathways are disrupted due to partial or total deficiency in sterol 27-hydroxylase.²⁴ Ctexli™ may act to replace deficient levels of the endogenous bile acids.²⁴

Advice to Patients

• For gallstone dissolution, inform patients of the importance of periodic visits for liver function tests and oral cholecystograms or ultrasonograms for monitoring stone dissolution.¹

• For treatment of cerebrotendinous xanthomatosis, inform the patient of the symptoms of hepatotoxicity (e.g., abdominal pain, bruising, dark-colored urine, fatigue, bleeding, jaundice, nausea, pruritus).²⁴ Instruct the patient to discontinue Ctexli™ immediately and seek medical care should symptoms occur.²⁴

• Inform patients of the importance of being aware of the symptoms of gallstone complications and of immediately reporting such symptoms to the clinician.¹

• Inform patients of the importance of long-term compliance with the dosage regimen; need for temporary dosage reduction if episodes of diarrhea occur.¹

• Advise patients to inform clinicians immediately if they are or plan to become pregnant or plan to breast-feed; necessity of advising patients to avoid pregnancy during therapy for gallstone dissolution.¹ Necessity of advising pregnant patients of the risk to the fetus when used for gallstone dissolution.¹

• Advise patients to inform clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.^{1 24}

• Inform patients of other important precautionary information.^{1 24}

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Ctexli™ is obtained through designated specialty pharmacies. Contact the manufacturer or consult the Ctexli™ website ([Web]) for specific availability information.²⁸

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