Benznidazole

Benznidazole is a nitroimidazole antimicrobial drug [see Microbiology ( 12.4 )] .

• Benznidazole Tablets are indicated in pediatric patients 2 to 12 years of age for the treatment of Chagas disease (American trypanosomiasis) caused by Trypanosoma cruzi . This indication is approved under accelerated approval based on the number of treated patients who became Immunoglobulin G (IgG) antibody negative against the recombinant antigens of T.

• • History of hypersensitivity reaction to benznidazole or other nitroimidazole derivatives ( 4.1 ). • Disulfiram usage within the last two weeks ( 4.2 ).contraindicated

Pediatric patients 2 to 12 years of age: The total daily dose is 5 mg/kg to 8 mg/kg orally administered in two divided doses separated by approximately 12 hours for a duration of 60 days ( 2.2 ). See Full Prescribing Information for important administration instructions ( 2.1 , 2.3 , 2.4 ). 2.1 Important Administration Instructions Benznidazole Tablets (12.5 mg and 100 mg) are for oral use and may be taken with or without food [see Clinical Pharmacology ( 12.3 )] . Benznidazole Tablets are dosed by body weight (kg) [see Dosage and Administration ( 2.2 )] . Benznidazole Tablets 100 mg are functionally scored tablets which can be split into one-half (50 mg) or one-quarter (25 mg) at the scored lines to provide doses less than 100 mg [see Instructions for Use ] . Benznidazole Tablets 12.5 mg and 100 mg can be made into slurry as an alternative method of administration [see Dosage and Administration ( 2.4 )] . 2.2 Recommended Dosage in Pediatric Patients (2 to 12 Years of Age) The total daily dose for pediatric patients 2 to 12 years of age is 5 mg/kg to 8 mg/kg orally administered in two divided doses separated by approximately 12 hours, for a duration of 60 days (see Table 1 ). Table 1: Recommended Dosage of Benznidazole Tablets in Pediatric Patients (2 to 12 Years of Age) Body Weight Range (kg) Dose (mg) Number of Benznidazole Tablets 12.5 mg Number of Benznidazole Tablets 100mg Duration and Frequency of Therapy Less than 15 kg 50 mg 4 tablets ½ tablet Administered twice daily approximately 12 hours apart for 60 days.

Potential Risk for Genotoxicity and Carcinogenicity ( 5.1 ). Embryo-Fetal Toxicity: Can cause fetal harm. Pregnancy testing is recommended for females of reproductive potential. Advise females of reproductive potential of the potential risk to a fetus and to use effective contraception ( 2.3 , 5.2 , 8.1 , 8.3 ). Hypersensitivity skin reactions have been reported with benznidazole. In case of skin reactions, presenting with additional symptoms of systemic involvement such as lymphadenopathy, fever and/or purpura, discontinuation of treatment is recommended ( 5.3 ). Treatment with Benznidazole Tablets can potentially cause paresthesia or symptoms of peripheral neuropathy. In cases where neurological symptoms occur, immediate discontinuation of treatment is recommended ( 5.4 ). There have been hematological manifestations of bone marrow depression, such as neutropenia, thrombocytopenia, anemia, and leukopenia ( 5.5 ). 5.1 Potential for Genotoxicity and Carcinogenicity Genotoxicity Genotoxicity of benznidazole has been demonstrated in humans, in vitro in several bacterial species and mammalian cell systems, and in vivo in rodents [see Nonclinical Toxicology ( 13.1 )] . A study evaluating the cytogenetic effect of benznidazole in pediatric patients ranging from 11 months to 11 years of age (the safety and effectiveness of Benznidazole Tablets in patients less than 2 years old has not been established) with Chagas disease demonstrated a two-fold increase in chromosomal aberrations.

The following serious and otherwise important adverse reactions are discussed in greater detail in other sections of labeling: Potential for Genotoxicity, Carcinogenicity, and Mutagenicity [see Warnings and Precautions ( 5.1 )] Hypersensitivity Skin Reactions [see Warnings and Precautions ( 5.3 )] Central and Peripheral Nervous System Effects [see Warnings and Precautions ( 5.4 )] Hematological Manifestations of Bone Marrow Depression [see Warnings and Precautions ( 5.5 )] Most common adverse reactions observed were abdominal pain, rash, decreased weight, headache, nausea, vomiting, neutropenia, urticaria, pruritus, eosinophilia, decreased appetite ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Exeltis USA, Inc. at 1-877-324-9349 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trial 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. Benznidazole was evaluated in two randomized, double-blind, placebo-controlled trials (Trial 1 1 and Trial 2 2 ) and one uncontrolled trial (Trial 3 3 ). Trial 1 was conducted in pediatric patients 6 to 12 years of age with chronic indeterminate Chagas disease in Argentina. The chronic indeterminate form includes patients with serologic evidence of T. cruzi infection without symptoms of cardiac or gastrointestinal disease.

Lactation: Breastfeeding is not recommended ( 8.2 ). 8.1 Pregnancy Risk Summary Based on findings from animal studies, Benznidazole Tablets may cause fetal harm when administered to a pregnant woman. Published postmarketing reports on benznidazole use during pregnancy are insufficient to inform a drug-associated risk of adverse pregnancy-related outcomes. There are risks to the fetus associated with Chagas Disease (see Clinical Considerations ) . In embryo-fetal development studies, benznidazole administered orally to pregnant rats and rabbits during organogenesis was associated with fetal malformations at doses approximately 1-3 times the MRHD in rats (anasarca, anophthalmia, and/or microphthalmia) and doses approximately 0.3-1.0 times the MRHD in rabbits (ventricular septal defect). In pregnant rats administered benznidazole during gestation and through lactation, effects in first generation offspring included reduced fertility in individual males and reduced numbers of live embryos and fetuses in pregnant females at a maternal dose equivalent to approximately 1.5 times the MRHD (see Data ) . Advise pregnant women of the potential risk to a fetus. 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.

Metabolism

Absorption The absorption of benznidazole from three different 100 mg benznidazole preparations was comparable when administered as a single dose under fasting conditions in adult healthy volunteers ( Table 6 ). Table 6: Summary of Benznidazole Pharmacokinetic (PK) Parameters Following a Single Oral Dose of 100 mg Benznidazole Administered Under Fasting Conditions in Adult Healthy Volunteers.

• Aug 29, 2017NDANDA209570Chemo Research Sl

1. 1Product Use Issue2022%
2. 2Rash1819%
3. 3Intentional Product Use Issue1718%
4. 4American Trypanosomiasis1314%
5. 5Nausea99.7%
6. 6Drug Ineffective88.6%
7. 7Headache88.6%
8. 8Drug Interaction66.5%
9. 9Dizziness55.4%
10. 10Hepatotoxicity55.4%
11. 11Off Label Use55.4%
12. 12Pruritus55.4%
13. 13Pyrexia55.4%
14. 14Cardiogenic Shock44.3%
15. 15Dyspnoea44.3%

The 10 most recently updated of 24 ClinicalTrials.gov registrations naming Benznidazole as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study of Efficacy, Safety, Tolerability of LXE408 in Participants With Chronic Chagas Disease.
  Recruiting · Phase 2 · Interventional · 130 enrolled · Novartis Pharmaceuticals
  NCT06632600updated 2026-06-01
• Prospective Study of Benznidazole for Chagas' Disease Children With Chronic Indeterminate Chagas Disease
  Active not recruiting · Phase 3 · Interventional · 178 enrolled · Insud Pharma
  NCT04024163updated 2026-04-21
• A Phase 1 Study of the Safety and Tolerability of ICM20 in Adults
  Completed · Phase 1 · Interventional · 13 enrolled · IC-MedTech Corporation
  NCT05523596updated 2026-04-16
• Short-course Benznidazole Treatment to Reduce Trypanosoma Cruzi Parasitic Load in Women of Reproductive Age
  Completed · Phase 3 · Interventional · 87 enrolled · Tulane University School of Public Health and Tropical Medicine
  NCT03672487updated 2026-04-09
• Short Benznidazole Regimen for Chronic Phase Chagas Disease Patients
  Withdrawn · Phase 3 · Interventional · 0 enrolled · Evandro Chagas Institute of Clinical Research
  NCT06339710updated 2025-03-13
• New Therapies and Biomarkers for Chagas Infection
  Completed · Phase 2 · Interventional · 450 enrolled · University of Texas, El Paso
  NCT03981523updated 2024-07-17
• Evaluation of Different Benznidazole Regimens for the Treatment of Chronic Chagas Disease.
  Completed · Phase 2 · Interventional · 238 enrolled · Hospital Universitari Vall d'Hebron Research Institute
  NCT03191162updated 2023-12-19
• Shorter Benznidazole Regimens Compared to the Standard Regimen for Chagas Disease
  Recruiting · Phase 3 · Interventional · 300 enrolled · Laboratorio Elea Phoenix S.A.
  NCT04897516updated 2023-11-30
• Nifurtimox Versus Benznidazole Effectiveness and Tolerance for Chagas Disease Treatment
  Unknown · Observational · 900 enrolled · Hospital de Niños R. Gutierrez de Buenos Aires
  NCT04274101updated 2023-03-01
• BENEFIT: Evaluation of the Use of Antiparasital Drug (Benznidazole) in the Treatment of Chronic Chagas' Disease
  Completed · Phase 3 · Interventional · 2,854 enrolled · Population Health Research Institute
  NCT00123916updated 2020-03-03

Frequently asked questions

How does Benznidazole work?

Benznidazole is a nitroimidazole antimicrobial drug [see Microbiology ( 12.4 )] .

What is Benznidazole used for?

According to FDA labeling, Benznidazole carries indications including: Benznidazole Tablets are indicated in pediatric patients 2 to 12 years of age for the treatment of Chagas disease (American trypanosomiasis) caused by Trypanosoma cruzi . This indication is approved under accelerated approval based on the number of treated patients who became Immunoglobulin G (IgG) antibody negative against the recombinant antigens of T.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Benznidazole?

Benznidazole is classified as Nitroimidazole derivatives, Unknown Cellular or Molecular Interaction, Decreased DNA Replication, Decreased Protein Synthesis, Decreased RNA Replication.

What are the contraindications for Benznidazole?

Benznidazole labeling lists contraindications including: • History of hypersensitivity reaction to benznidazole or other nitroimidazole derivatives ( 4.1 ). • Disulfiram usage within the last two weeks ( 4.2 ).. Always consult the full prescribing information and a clinician.