BENDITA BEnznidazole New Doses Improved Treatment and Associations

NCT ID: NCT03378661

Last Updated: 2017-12-20

Study Results

Results pending

The study team has not published outcome measurements, participant flow, or safety data for this trial yet. Check back later for updates.

Basic Information

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Recruitment Status

UNKNOWN

Clinical Phase

PHASE2

Total Enrollment

210 participants

Study Classification

INTERVENTIONAL

Study Start Date

2016-11-30

Study Completion Date

2018-07-27

Brief Summary

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Recent scientific advances have provided further impetus to develop new therapeutic approaches for Chagas Disease (CD) using different doses and duration of BZN, as well as combinations directed at multiple therapeutic targets to improve treatment response and tolerability and reduce the potential for development of resistance.

This project focuses on the proof-of-concept evaluation of improved treatment regimens of BZN, with the assessment of new BZN-sparing regimens in monotherapy and in combination with E1224.

Detailed Description

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The current treatment for Chagas disease has significant limitations, including long treatment durations, safety and tolerability concerns and is currently limited to two nitro-heterocyclic drugs, nifurtimox and benznidazole (BZN). BZN, a nitroimidazole introduced by Roche in 1971, is marketed by Laboratório Farmacêutico do Estado de Pernambuco S/A - LAFEPE and Laboratorio ELEA - Argentina. It is supplied in tablets strengths of 12.5, 50 and 100 mg, administered twice daily at a dose of 5 mg/kg body weight/day for adults and 5-10 mg/kg body weight/day for children for 30-60 days. Notably, the current regimens with BZN for the treatment of adults with CD likely represent the maximum dosing case scenario in terms of dose, duration and schedule of administration (Chagas expert meeting DNDi. January 2014. GVA).

Doses and duration of treatment for CD have not been evaluated systematically. Current treatment regimens and dosing intervals have been derived from decades-old patient series and with very limited direct comparisons. Data from recently concluded trials suggest existing opportunities for optimisation of the treatment regimens of BZN.

A (Drugs for Neglected Disease initiative) DNDi-sponsored Phase 2, proof-of-concept clinical trial on E1224 and Benznidazole (BZN) in adults with chronic indeterminate CD, conducted between 2011 and 2013 in Bolivia, showed that all BZN-treated patients had cleared parasite DNA after 2 weeks of treatment and 81% sustained the parasite clearance at 12 months after treatment. At end-of treatment (EOT, Day 65), E1224 was found to be efficacious in clearing T. cruzi parasites when compared to placebo. However, at 12 months less than one third of patients sustained parasite clearance. The trial safety data also indicated a proportion of patients (10-20%) who do not complete treatment in conditions of use, the majority due to adverse drug reactions (ADRs) and the long treatment duration.

Taking into consideration the efficacy gap with about 80% sustained response and a tolerability gap, with a proportion of patients (10-20%) who do not complete treatment, two approaches for Chagas treatment optimization are to be pursued:

1. A change in the current adult dosing regimen for BNZ to reduce exposure and improve tolerability while maintaining efficacy; and
2. The development of a combination therapy to improve efficacy while maintaining or improving tolerability. The combination therapy aims to address the efficacy gap and may or may not address tolerability gap.

With regards to the dosing regimen, population-pharmacokinetics studies observed BZN plasma concentrations in children were significantly lower than those previously reported in adults (treated with comparable mg/kg doses). At the same time, all children had parasite clearance, few adverse reactions to the drug. Recent population PK data in adults suggested that the current BZN dosing regimen (2.5 mg/kg/12 h) may lead to overexposure in the majority of patients. Dosing simulations suggested that a BNZ dose of 2.5 mg/kg/24 h would adequately keep BNZ trough plasma concentrations within the recommended target range for the majority of patients. There are also opportunities for evaluation of fixed dose regimens for adult dosing, rather than mg/kg calculations, with increased ease-of-use and potential for improved compliance in scaling up treatment of CD. Intermittent dosing regimens was also evaluated in murine model of chronic CD and in a pilot follow-up trial with 17 adult patients with chronic CD was, with similar parasitological cure rates to standard treatment.

Likewise, several controlled observational trials with BZN, 5 mg/kg/day for 30 or 60 days have shown a reduction in the progression of heart disease serological and sero-negative conversion up to 60% in children and 30% in adults. Different publications showed anti-parasitic efficacy of treatment regimens with 30 and 60 days, and of incomplete treatment of 10 days. Combination therapy is a well-recognized treatment modality in many disease settings, including cancer, cardiovascular disease, and infectious diseases. Several infectious diseases such as tuberculosis, malaria, leprosy, and AIDS only came under control and were effectively treated after introduction of combinations of drugs that utilize different mechanisms of action.

E1224 is a water-soluble monolysine salt form of the ravuconazole (RAV) pro-drug (which is a phosphonooxymethyl ether derivative of RAV). It is a broad-spectrum triazole antifungal.

Pooled safety data for the monolysine prodrug E1224 from Phase 1 and 2 trials indicated that E1224 was generally well tolerated and exhibited a safety profile quite similar to other azoles. Adverse events occurring in greater than 3% of E1224 recipients, with a dose-dependent pattern and at rates higher than those observed in placebo recipients included nausea, abnormalities in liver enzymes, dizziness, anxiety, and contact dermatitis.

Safety evaluations indicated relatively mild, transient, and asymptomatic increases in liver enzymes - completely reversible upon discontinuation of therapy. Phase 1 cardiac safety evaluations showed that E1224 administration did not result in QTc interval prolongation.

Experimental data suggest a positive interaction between BZN and azole compounds for the treatment of Chagas disease.18 A Phase 1 drug-drug interaction trial was designed to assess the pharmacokinetics (PK) and safety interaction of BNZ and E1224 co-administered daily for a total of 54 days (Day 4 to Day 15- E1224 multiple dose 400 mg loading dose once daily for 3 days, followed by maintenance dose 100mg once daily for 9 days (from Day 7 to Day 15); Day 9 BNZ single dose (2.5 mg/kg); and Day 12 to Day 15 BNZ multiple dose (2.5 mg/kg twice daily)). The trial was conducted in Argentina and was concluded in early 2015, with enrolment of 28 healthy male volunteers. Both compounds were well tolerated, in monotherapy and combination. There were no treatment discontinuations or serious adverse events. Transient, minor, non-concomitant increase in bilirubin and liver transaminases occurred in 2 patients in a pattern not suggestive of drug effect. There was no interaction of RAV on BNZ PK and the limited impact of BNZ on RAV PK, suggesting that co-administration of RAV and BNZ may not require any E1224 dosing adaptation. The lack of clinically relevant safety findings provided support for follow-up evaluation of the two compounds in combination.

In conclusion, recent scientific advances have provided further impetus to develop new therapeutic approaches for CD using different doses and duration of BZN, as well as combinations directed at multiple therapeutic targets to improve treatment response and tolerability and reduce the potential for development of resistance.

This project focuses on the proof-of-concept evaluation of improved treatment regimens of BZN, with the assessment of new BZN-sparing regimens in monotherapy and in combination with E1224.

Conditions

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Chagas Disease

Keywords

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Chronic, Indeterminate

Study Design

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Allocation Method

RANDOMIZED

Intervention Model

PARALLEL

Parallel Assignment
Primary Study Purpose

TREATMENT

Blinding Strategy

QUADRUPLE

Participants Caregivers Investigators Outcome Assessors
Double Dummy

Study Groups

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BZN STD Regimen

Benznidazole (100 mg and 50 mg) tablets by mouth, every 12 hours for 8 weeks.

Three E1224 Placebo 100 mg capsules by mouth, everyday on days 1 to 3, followed by three E1224 Placebo 100 mg capsules by mouth, once weekly (starting on week 2) for 7 weeks.

Group Type EXPERIMENTAL

Benznidazole

Intervention Type DRUG

Benznidazole tablet

E1224 Placebo

Intervention Type DRUG

E1224 matched placebo capsules

BZN 300 mg - 4 wks

Benznidazole (100 mg and 50 mg) tablets by mouth, every 12 hours for 4 weeks, followed by:

Benznidazole Placebo (100 mg and 50 mg) tablets by mouth, every 12 hours for 4 weeks.

Three E1224 Placebo 100 mg capsules by mouth, everyday on days 1 to 3, followed by three E1224 Placebo 100 mg capsules by mouth, once weekly (starting on week 2) for 7 weeks.

Group Type EXPERIMENTAL

Benznidazole

Intervention Type DRUG

Benznidazole tablet

E1224 Placebo

Intervention Type DRUG

E1224 matched placebo capsules

Benznidazole Placebo

Intervention Type DRUG

Benznidazole matched placebo tablets

BZN 300 mg - 2 wks

Benznidazole (100 mg and 50 mg) tablets by mouth, every 12 hours for 2 weeks, followed by:

Benznidazole Placebo (100 mg and 50 mg) tablets by mouth, every 12 hours for 6 weeks.

Three E1224 Placebo 100 mg capsules by mouth, everyday on days 1 to 3, followed by three E1224 Placebo 100 mg capsules by mouth, once weekly (starting on week 2) for 7 weeks.

Group Type EXPERIMENTAL

Benznidazole

Intervention Type DRUG

Benznidazole tablet

E1224 Placebo

Intervention Type DRUG

E1224 matched placebo capsules

Benznidazole Placebo

Intervention Type DRUG

Benznidazole matched placebo tablets

BZN 150 mg - 4 wks

Benznidazole (100 mg and 50 mg) tablets and Benznidazole Placebo (100 mg and 50 mg) tablets by mouth, in two separate daily doses for 4 weeks, followed by:

Benznidazole Placebo (100 mg and 50 mg) tablets by mouth, every 12 hours for 4 weeks.

Three E1224 Placebo 100 mg capsules by mouth, everyday on days 1 to 3, followed by three E1224 Placebo 100 mg capsules by mouth, once weekly (starting on week 2) for 7 weeks.

Group Type EXPERIMENTAL

Benznidazole

Intervention Type DRUG

Benznidazole tablet

E1224 Placebo

Intervention Type DRUG

E1224 matched placebo capsules

Benznidazole Placebo

Intervention Type DRUG

Benznidazole matched placebo tablets

BZN 150 mg - 4 wks / E1224 300 mg

Benznidazole (100 mg and 50 mg) tablets and Benznidazole Placebo (100 mg and 50 mg) tablets by mouth, in two separate daily doses for 4 weeks, followed by:

Benznidazole Placebo (100 mg and 50 mg) tablets by mouth, every 12 hours for 4 weeks.

Three E1224 100 mg capsules by mouth, everyday on days 1 to 3, followed by three E1224 100 mg capsules by mouth, once weekly (starting on week 2) for 7 weeks. (total dose: 3000 mg).

Group Type EXPERIMENTAL

Benznidazole

Intervention Type DRUG

Benznidazole tablet

E1224

Intervention Type DRUG

E1224 capsules

Benznidazole Placebo

Intervention Type DRUG

Benznidazole matched placebo tablets

BZN 300 mg (weekly) 8 wks / E1224 300 mg

Benznidazole (100 mg and 50 mg) tablets by mouth, once weekly for 8 weeks (total 8 days of intermittent treatment) and Benznidazole Placebo (100 mg and 50 mg) tablets by mouth, in the other 6 days of the week for 8 weeks

Three E1224 100 mg capsules by mouth, everyday on days 1 to 3, followed by three E1224 100 mg capsules by mouth, once weekly (starting on week 2) for 7 weeks. (total dose: 3000 mg).

Group Type EXPERIMENTAL

Benznidazole

Intervention Type DRUG

Benznidazole tablet

E1224

Intervention Type DRUG

E1224 capsules

Benznidazole Placebo

Intervention Type DRUG

Benznidazole matched placebo tablets

Placebo

Benznidazole Placebo (100 mg and 50mg) tablets by mouth, every 12 hours for 8 weeks.

Three E1224 Placebo 100 mg capsules by mouth, everyday on days 1 to 3, followed by three E1224 Placebo 100 mg capsules by mouth, once weekly (starting on week 2) for 7 weeks.

Group Type PLACEBO_COMPARATOR

E1224 Placebo

Intervention Type DRUG

E1224 matched placebo capsules

Benznidazole Placebo

Intervention Type DRUG

Benznidazole matched placebo tablets

Interventions

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Benznidazole

Benznidazole tablet

Intervention Type DRUG

E1224

E1224 capsules

Intervention Type DRUG

E1224 Placebo

E1224 matched placebo capsules

Intervention Type DRUG

Benznidazole Placebo

Benznidazole matched placebo tablets

Intervention Type DRUG

Other Intervention Names

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Abarax® N-benzil-2-nitro-1-imidazolacetamide) Lafepe Benznidazol ABALEA® Fosravuconazole E1224 (prodrug for active ingredient Ravuconazole) Placebo (for E1224) Placebo (for Benznidazole)

Eligibility Criteria

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Inclusion Criteria

* Confirmed diagnosis of T. cruzi infection by: Serial qualitative PCR (three samples collected over a single day, at least one of which must be positive) AND Conventional serology (a minimum of two positive tests must be positive \[Conventional ELISA, Recombinant Elisa and/or IIF)
* Women in reproductive age must have a negative serum pregnancy test at screening, must not be breastfeeding, and must use a double barrier method of contraception to avoid pregnancy throughout a clinical trial and for 3 months after completion of the trial, in such a manner that the risk of pregnancy is minimized especially during exposure to treatment. Women who are using oral, implanted, or injectable contraceptive hormones or mechanical products such as an intrauterine device with a hormonal component are required to use an additional barrier method of contraception for the time period specified.
* Normal EKG (PR ≤200 msec, QRS \<120 msec, and QTc ≥350 msec and ≤450 msec interval durations in males and QTc ≤470 msec in women) at screening.

Exclusion Criteria

The presence of any of the following will exclude a patient from trial randomization:

* Signs and/or symptoms of chronic cardiac and/or digestive form of CD
* History of cardiomyopathy, heart failure, or ventricular arrhythmia.
* History of digestive surgery or mega syndromes.
* Any other acute or chronic health conditions that, in the opinion of the PI, may interfere with the efficacy and/or safety evaluation of the trial drug (such as acute infections, history of HIV infection, diabetes, uncontrolled systolic/diastolic blood pressure, liver, and renal disease requiring medical treatment).
* Laboratory test values considered clinically significant or out of the allowable range at selection period as follows:
* Total WBC must be within the normal range, with an acceptable margin of +/- 5% (3,800 - 10,500/mm3).
* Platelets must be within the normal range up to 550,000/mm3
* Total bilirubin must be within the normal range
* Transaminases (ALT and AST) must be within the normal range, with an acceptable margin of 25% above the upper limit of normality (ULN), \<1.25 x ULN.
* Creatinine must be within an acceptable margin of 10% above the ULN, \<1.10 x ULN.
* Alkaline phosphatase must be within the normal range up to Grade 1 CTCAE (\< 2.5 x ULN)
* GGT must be within the normal range up to 2x ULN.
* Fasting glucose must be within the normal range
* Electrolytes (Ca, Mg, K) must be within the normal range
* If the results of the blood tests (hematology and biochemistry) are out of the ranges defined above, but within the limits of CTCAE (version 4.03) Grade 1, and the laboratory finding is considered as non-clinically significant, a new sample can be collected for a retest. Only one retest will be allowed within the screening period.
* If the result of retest is within the margins defined above, the Investigator will review the parameter(s) together with all other medical information available (medical history, clinical examinations, vital signs, etc.) and upon his/her medical judgment will decide if the patient is eligible or not for trial randomization.
* Any condition that prevents the patient from taking oral medication
* Patients with history of allergy (serious or not), allergic skin rash, asthma, intolerance, sensitivity or photosensitivity to any drug
* Patients with any contra-indication (known hypersensitivity) to any nitroimidazoles, e.g. metronidazole.
* Any concomitant use of allopurinol, antimicrobial, or anti-parasitic agents.
* Any planned surgery likely to interfere with the trial conduction and/or treatment evaluation
* Unlikely to co-operate with the trial
* Any previous participation in any clinical trial for Chagas Disease treatment evaluation
* Participation in another trial at the same time or within 3 months prior to selection (according to local regulations)
Minimum Eligible Age

18 Years

Maximum Eligible Age

50 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

No

Sponsors

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Drugs for Neglected Diseases

OTHER

Sponsor Role lead

Responsible Party

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Responsibility Role SPONSOR

Principal Investigators

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Faustino Torrico, PhD

Role: PRINCIPAL_INVESTIGATOR

Plataforma de Atención Integral de Pacientes con Enfermedad de Chagas. Cochabamba, Bolivia.

Joaquim Gascón, PhD

Role: PRINCIPAL_INVESTIGATOR

Centro de Salud Internacional, Hospital Clínico de Barcelona CRESIB - Centre de Recerca en Salut Internacional de Barcelona Barcelona, España.

Locations

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Plataforma de Atención Integral de Pacientes con Enfermedad de Chagas.

Sucre, Chuquisaca Department, Bolivia

Site Status

Plataforma de Atención Integral de Pacientes con Enfermedad de Chagas.

Cochabamba, , Bolivia

Site Status

Plataforma de Atención Integral de Pacientes con Enfermedad de Chagas.

Tarija, , Bolivia

Site Status

Countries

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Bolivia

References

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Saade U, de Boer J, Scandale I, Altcheh J, Pottel H, Chatelain E, Zrein M. Early assessment of antibodies decline in Chagas patients following treatment using a serological multiplex immunoassay. Nat Commun. 2024 Dec 3;15(1):10530. doi: 10.1038/s41467-024-54910-x.

Reference Type DERIVED
PMID: 39627222 (View on PubMed)

Torrico F, Gascon J, Barreira F, Blum B, Almeida IC, Alonso-Vega C, Barboza T, Bilbe G, Correia E, Garcia W, Ortiz L, Parrado R, Ramirez JC, Ribeiro I, Strub-Wourgaft N, Vaillant M, Sosa-Estani S; BENDITA study group. New regimens of benznidazole monotherapy and in combination with fosravuconazole for treatment of Chagas disease (BENDITA): a phase 2, double-blind, randomised trial. Lancet Infect Dis. 2021 Aug;21(8):1129-1140. doi: 10.1016/S1473-3099(20)30844-6. Epub 2021 Apr 6.

Reference Type DERIVED
PMID: 33836161 (View on PubMed)

Other Identifiers

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DNDi-CH-E1224-003

Identifier Type: -

Identifier Source: org_study_id