Evaluating the Safety and Drug Interaction of PA-824, an Investigational Tuberculosis Medication, Together With Efavirenz, Ritonavir-Boosted Lopinavir, or Rifampin

NCT ID: NCT01571414

Last Updated: 2021-11-05

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

COMPLETED

Clinical Phase

PHASE1

Total Enrollment

52 participants

Study Classification

INTERVENTIONAL

Study Start Date

2012-05-31

Study Completion Date

2013-05-31

Brief Summary

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Tuberculosis (TB) is a global public health concern and developing new treatment regimens is an important research priority. PA-824 is an experimental TB medication. This study will evaluate the safety and tolerability of PA-824 when combined with efavirenz (EFV) or ritonavir-boosted lopinavir (LPV/r), which are medications used to treat HIV infection, or rifampin (RIF), which is a medication used to treat TB. Study researchers will examine the safety and tolerability of these drug combinations and how the medications affect the levels of PA-824 in the blood.

Detailed Description

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TB is a global public health threat. In 2009, there were an estimated 9.4 million cases of TB and 1.8 million deaths from the disease. TB treatment regimens are often lengthy and complex, and multidrug-resistant (MDR) TB is emerging as a worldwide epidemic. TB is also one of the most common causes of death among people infected with HIV. PA-824 is an experimental drug developed for the treatment of TB. This study will evaluate the safety, tolerability, and pharmacokinetic (PK) drug interactions between PA-824 and EFV, LPV/r, or RIF.

This study will enroll healthy adults who are not infected with HIV or TB. Participants will be enrolled into one of three arms, with Arms 1 and 2 each consisting of two groups. Participants in Arm 1 will be randomly assigned to receive PA-824 alone or EFV alone followed by EFV plus PA-824 in one of two sequences. Participants in Arm 2 will be randomly assigned to receive PA-824 alone or LPV/r alone followed by LPV/r plus PA-824 in one of two sequences. For participants in Arms 1 and 2, there will be a 14-day washout period between treatments, where participants will not receive any medication. Participants in Arm 3 will receive PA-824 alone, followed by RIF alone, and then RIF plus PA-824. Participants in Arms 1 and 2 will attend outpatient study visits at study entry and either Days 3, 22, and 29 or Days 7, 36, and 39, depending on which group they are in. Participants in Arm 3 will attend outpatient study visits at study entry and Days 3, 10, and 15. At most study visits, participants will undergo a physical examination, vital sign measurements, medication and medical history review, and blood collection. Participants will complete a medication and symptom diary throughout the study.

All participants also will be admitted to an inpatient clinical research unit two or three times during the study, depending on which arm they are enrolled in. Each inpatient visit will last 1 or 2 days. During the inpatient visits, participants will undergo several blood collections throughout the day; select visits also will include an electrocardiogram (ECG).

Participants in Arms 1 and 2 will receive the last dose of their assigned medication on Day 42. Participants in Arm 3 will receive the last dose of their assigned medication on Day 21. A final study visit will occur for all participants 1 to 2 weeks later.

Conditions

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Tuberculosis

Study Design

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Allocation Method

RANDOMIZED

Intervention Model

CROSSOVER

Primary Study Purpose

TREATMENT

Blinding Strategy

NONE

Study Groups

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Arm 1A-EFV and PA-824

Participants will receive PA-824 on Days 1 to 7, no study medication on Days 8 to 21, EFV on Days 22 to 35, and EFV plus PA-824 on Days 36 to 42. Inpatient study visits will occur at Days 7, 34, and 41 to 42.

Group Type EXPERIMENTAL

PA-824

Intervention Type DRUG

200-mg tablets once a day

Efavirenz (EFV)

Intervention Type DRUG

600-mg tablets once a day

Arm 1B-EFV and PA-824

Participants will receive EFV on Days 1 to 14, EFV plus PA-824 on Days 15 to 21, no study medication on Days 22 to 35, and PA-824 on Days 36 to 42. Inpatient study visits will occur at Days 13, 20 to 21, and 42.

Group Type EXPERIMENTAL

PA-824

Intervention Type DRUG

200-mg tablets once a day

Efavirenz (EFV)

Intervention Type DRUG

600-mg tablets once a day

Arm 2A-LPV/r and PA-824

Participants will receive PA-824 on Days 1 to 7, no study medication on Days 8 to 21, LPV/r on Days 22 to 35, and LPV/r plus PA-824 on Days 36 to 42. Inpatient study visits will occur at Days 7, 35, and 42.

Group Type EXPERIMENTAL

PA-824

Intervention Type DRUG

200-mg tablets once a day

Lopinavir/Ritonavir (LPV/r)

Intervention Type DRUG

400-mg/100-mg tablets twice a day

Arm 2B-LPV/r and PA-824

Participants will receive LPV/r on Days 1 to 14, LPV/r plus PA-824 on Days 15 to 21, no study medication on Days 22 to 35, and PA-824 on Days 36 to 42. Inpatient study visits will occur at Days 14, 21, and 42.

Group Type EXPERIMENTAL

PA-824

Intervention Type DRUG

200-mg tablets once a day

Lopinavir/Ritonavir (LPV/r)

Intervention Type DRUG

400-mg/100-mg tablets twice a day

Arm 3-RIF and PA-824

Participants will receive PA-824 on Days 1 to 7, RIF on Days 8 to 14, and RIF plus PA-824 on Days 15 to 21. Inpatient study visits will occur at Days 7 and 21.

Group Type EXPERIMENTAL

PA-824

Intervention Type DRUG

200-mg tablets once a day

Rifampin (RIF)

Intervention Type DRUG

300-mg capsules once a day

Interventions

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PA-824

200-mg tablets once a day

Intervention Type DRUG

Efavirenz (EFV)

600-mg tablets once a day

Intervention Type DRUG

Lopinavir/Ritonavir (LPV/r)

400-mg/100-mg tablets twice a day

Intervention Type DRUG

Rifampin (RIF)

300-mg capsules once a day

Intervention Type DRUG

Eligibility Criteria

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Inclusion Criteria

* Contraception requirements: Females of reproductive potential must have a negative serum or urine beta-human choriogonadotropin (β-HCG) pregnancy test performed within 48 hours before study entry. All participants must agree not to participate in a conception process (e.g., active attempt to become pregnant or to impregnate, sperm donation, in vitro fertilization). If participating in sexual activity that could lead to pregnancy, participants must agree to use two reliable forms of contraceptives simultaneously while on study and for a number of weeks after the final study visit as defined in the protocol. More information on this criterion can be found in the protocol.
* Able and willing to provide written informed consent
* Absence of HIV-1 infection, as documented by any licensed enzyme-linked immunosorbent assay (ELISA) test kit, within 21 days prior to study entry
* Creatinine clearance of greater than 50 mL/min, within 21 days prior to study entry, calculated by the Cockcroft-Gault method. More information on this criterion can be found in the protocol.
* Laboratory values obtained within 21 days prior to study entry:

1. Hemoglobin greater than 12 g/dL for men and greater than 11 g/dL for women
2. Platelet count greater than or equal to 125,000/cu mm
3. Absolute neutrophil count greater than or equal to 1,250/cu mm
4. Serum albumin greater than or equal to the lower limit of normal for the laboratory
5. Serum potassium greater than or equal to the lower limit of normal and less than or equal to the upper limit of normal for the laboratory
6. Serum alanine aminotransferase (ALT) less than or equal to the upper limit of normal (ULN) for the laboratory
* Note: Screening laboratory evaluations may be repeated if one or more of the values are out of range. It is preferable, although not required, for prospective participants to fast (i.e., nothing by mouth \[NPO\] except water) for 4 hours prior to drawing samples for screening serum albumin, serum potassium, and serum ALT evaluations.
* Hepatitis B surface antigen negative, performed by a Clinical Laboratory Improvement Amendments (CLIA)-certified laboratory within 21 days prior to study entry
* Hepatitis C virus (HCV) antibody negative or, if the participant is known to have a positive hepatitis C antibody test, negative HCV RNA test, performed by a CLIA-certified laboratory within 21 days prior to study entry

Exclusion Criteria

* Use of any prescription or nonprescription medication known to inhibit or induce CYP3A or CYP2B6 metabolizing enzymes (refer to the manufacturers' package inserts for individual drugs) within 30 days prior to study entry
* Planned use during the study, from study entry through the last PK blood draw, of any of the following: prescription medication(s) \[excluding IUDs that elute locally active hormonal contraceptives\], herbal supplement(s), nutritional supplement(s), or over-the-counter medication(s). Note: Multivitamins, acetaminophen (up to 650 mg every 6 hours as an analgesic), ibuprofen (up to 600 mg twice daily), naproxen (up to 500 mg twice daily for pain or headache), and diphenhydramine (up to 25 mg daily for insomnia or seasonal allergies) are permitted.
* Hospitalization for any reason within 14 days prior to study entry
* Pharmacotherapy for serious illness within 14 days prior to study entry
* Use of any prescription medication(s) within 14 days prior to study entry
* Receipt of any investigational study drug, vaccine, or treatment within 21 days prior to study entry
* Known allergy/sensitivity or any hypersensitivity to PA-824, EFV, LPV, RTV, RIF, or components of their formulations
* As determined by the site investigator, a significant previous or active history of cardiovascular, renal, liver, hematologic, neurologic, gastrointestinal, psychiatric, endocrine, or immunologic disease(s); this is inclusive of chronic illnesses or gastrointestinal conditions that may affect drug absorption, etc.
* Any medical condition that, in the opinion of the site investigator, would interfere with the participant's ability to participate in the study
* Active illicit drug use or dependence that, in the opinion of the site investigator, would interfere with adherence to study requirements
* Clinical evidence of active TB. Note: Clinical evidence of active TB is based on history and physical examination. No other screening tests for TB are required for the study.
* Inability to abstain from consuming alcoholic beverages during defined periods throughout the study and grapefruits, mandarin oranges, and grapefruit juice for the entire duration of the study. Note: Participants are permitted to consume alcoholic beverages only during the washout period of Arms 1 and 2. Participants must agree to abstain from consuming alcoholic beverages for the duration of Arm 3.
* For smokers, inability to smoke less than or equal to 5 cigarettes per day for the entire duration of the study
* Breastfeeding
* ECG showing first-degree or greater heart block or QTc greater than 450 ms within 21 days prior to study entry. More information on this criterion can be found in the protocol.
* Frequent or severe headaches, defined as more than two headaches per week on average during the last 30 to 60 days prior to study entry or headaches greater than or equal to once every 30 days during the last 90 days prior to study entry that were severe enough to interfere with activities of daily living or ability to work or carry out daily responsibilities
Minimum Eligible Age

18 Years

Maximum Eligible Age

65 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

Yes

Sponsors

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National Institute of Allergy and Infectious Diseases (NIAID)

NIH

Sponsor Role lead

Responsible Party

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Responsibility Role SPONSOR

Principal Investigators

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Kelly E. Dooley, MD, PhD

Role: STUDY_CHAIR

Johns Hopkins University

Locations

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Ucsf Hiv/Aids Crs

San Francisco, California, United States

Site Status

Johns Hopkins University CRS

Baltimore, Maryland, United States

Site Status

Ohio State University CRS

Columbus, Ohio, United States

Site Status

Vanderbilt Therapeutics (VT) CRS

Nashville, Tennessee, United States

Site Status

Countries

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United States

References

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Dooley KE, Luetkemeyer AF, Park JG, Allen R, Cramer Y, Murray S, Sutherland D, Aweeka F, Koletar SL, Marzan F, Bao J, Savic R, Haas DW; AIDS Clinical Trials Group A5306 Study Team. Phase I safety, pharmacokinetics, and pharmacogenetics study of the antituberculosis drug PA-824 with concomitant lopinavir-ritonavir, efavirenz, or rifampin. Antimicrob Agents Chemother. 2014 Sep;58(9):5245-52. doi: 10.1128/AAC.03332-14. Epub 2014 Jun 23.

Reference Type DERIVED
PMID: 24957823 (View on PubMed)

Lenaerts AJ, Gruppo V, Marietta KS, Johnson CM, Driscoll DK, Tompkins NM, Rose JD, Reynolds RC, Orme IM. Preclinical testing of the nitroimidazopyran PA-824 for activity against Mycobacterium tuberculosis in a series of in vitro and in vivo models. Antimicrob Agents Chemother. 2005 Jun;49(6):2294-301. doi: 10.1128/AAC.49.6.2294-2301.2005.

Reference Type BACKGROUND
PMID: 15917524 (View on PubMed)

Singh R, Manjunatha U, Boshoff HI, Ha YH, Niyomrattanakit P, Ledwidge R, Dowd CS, Lee IY, Kim P, Zhang L, Kang S, Keller TH, Jiricek J, Barry CE 3rd. PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release. Science. 2008 Nov 28;322(5906):1392-5. doi: 10.1126/science.1164571.

Reference Type BACKGROUND
PMID: 19039139 (View on PubMed)

Other Identifiers

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11829

Identifier Type: REGISTRY

Identifier Source: secondary_id

ACTG5306

Identifier Type: -

Identifier Source: secondary_id

A5306

Identifier Type: -

Identifier Source: org_study_id