Overview

Impact of Steady State Cobicistat and Darunavir/Cobicistat on the Pharmacokinetics and Pharmacodynamic of Oral Anticoagulants (Rivaroxaban, Apixaban) in Health Volunteers

Status:
Recruiting
Trial end date:
2022-12-31
Target enrollment:
0
Participant gender:
All
Summary
Background: Rivaroxaban and apixaban are blood thinners. People with HIV may need to take them to treat or prevent blood clots. The anti-HIV drug darunavir (DRV) can increase the amount of these blood thinners in the body. This can cause bleeding or other health problems. The drug cobicistat (COBI) is used to help anti-HIV drugs work better. Researchers want to give healthy people DRV combined with COBI to learn how it affects rivaroxaban or apixaban blood levels. Objective: To test blood levels of rivaroxaban or apixaban when taken with COBI and DRV/COBI. Eligibility: Healthy volunteers ages 18-65 Design: Participants will be screened with: Medical history Physical exam Fasting blood and urine tests. (Urine tests will be performed in females of child-bearing potential only) Participants will have 8 visits; 3 are long (about 10-12 hours) and 5 are about 1 hour. They include: Baseline and final visits: Fasting blood and urine tests Day 1 visit (long day): Fasting blood and urine tests Catheter placement: A needle will insert a small tube into the participant s arm vein. Blood will be drawn up to 10 times. Dose of rivaroxaban or apixaban Day 2 visit (short day): Fasting blood tests Dose of COBI Participants will receive a bottle containing COBI tablets to take at home. Day 7 (long day): Fasting blood and urine tests Catheter placement: A needle will insert a small tube into the participant s arm vein. Blood will be drawn up to 10 times. Dose of rivaroxaban or apixaban Dose of COBI Day 8 (short day): Fasting blood tests Dose of DRV/COBI Participants will receive a bottle containing DRV/COBI tablets to take at home. Day 13 (long day): Fasting blood and urine tests Catheter placement: A needle will insert a small tube into the participant s arm vein. Blood will be drawn up to 10 times. Dose of rivaroxaban or apixaban Dose of DRV/COBI Day 14 (short day): Fasting blood tests Participants will take COBI tablets daily at home on days 3-6, and DRV/COBI on days 9 -12 during the study. They will record doses and side effects. During the study, participants cannot: Take most medications. Drink alcohol, smoke, or vape Engage in activities such as contact and extreme sports
Phase:
Phase 1
Accepts Healthy Volunteers?
Accepts Healthy Volunteers
Details
Lead Sponsor:
National Institutes of Health Clinical Center (CC)
Treatments:
Anticoagulants
Apixaban
Cobicistat
Cobicistat mixture with darunavir
Darunavir
Rivaroxaban
Criteria
- INCLUSION CRITERIA:

A subject will be considered eligible for this study only if all of the following criteria
are met:

- Adults between the ages of 18 to 65 years.

- Body mass index between 18 to 30 kg/M(2).

- Judged to be healthy based on medical history, physical examination, vital signs and
clinical laboratory tests (liver function tests (LFTs: alanine transaminase [ALT],
aspartate transaminase (AST), total bilirubin less than or equal to upper limit of
normal [ULN] (with the exception of participants with Gilbert s syndrome), albumin
within normal limits (WNL)], eGFR > 90 mL/min/1.73 m(2), PLT>150,000/microL,
hemoglobin (Hgb) greater than or equal to 12 g/dL, aPTT less than or equal to ULN, PTT
less than or equal to ULN, INR less than or equal to ULN.

- Subject agrees to storage of specimens for future research.

- Negative serum or urine pregnancy test for females of child-bearing potential.

- For female subjects, willing to avoid pregnancy by (a) practicing abstinence or (b)
using effective non-hormonal and/or barrier methods of birth control, as well as avoid
breast feeding or providing breast milk to infant during the study period. (baseline
visit up to end of study day 20 plus minus 3)

- Willing to avoid engaging in activities such as contact sports, including extreme
sports, that may increase the risk of bleeding through body injury or bruising, during
the study period (baseline visit up to end of study day 20 plus minus 3)

- Willingness to forgo drinking alcohol during the study period (baseline visit up to
end of study day 20 plus minus 3)

- Able to provide consent.

EXCLUSION CRITERIA:

A subject will be ineligible for this study if one, or more, of the following criteria are
met:

- HIV infection, as determined by standard serologic or virologic assays for HIV
infection.

- Laboratory evidence of active or chronic hepatitis A, B or C infection.

- History or presence of any of the following:

- any major medical conditions that requires daily frequent medication or
potentially impairs medication absorption, metabolism and elimination

- any other condition that may interfere with the interpretation of the study
results, or not be in the best interest of the subject in the opinion of the
Investigator.

- Current participation in an ongoing investigational drug protocol or use of any
investigational drug within 30 days (based on last dose received) prior to receipt of
any study drugs/medications.

- History or presence of the following:

- bleeding/hematologic disorders (e.g., anemia, hemophilia, etc.),

- serious/major bleeding event (intracranial, gastrointestinal (GI), as assessed by
subject interview), or

- current increased risk of bleeding

- for female subjects, menorrhagia

- Planned invasive or surgical procedure within (prior to or following) 28 days of study
participation.

- Therapy with any prescription, over-the-counter, herbal, or holistic medications,
including hormonal contraceptives by any route, within 5 half-lives of the agent prior
to receipt of any study medications will not be permitted with the following
exception:

Intermittent or short-course therapy (<14 days) with prescription, vaccines or
over-the-counter medications will be reviewed by investigators on a case-by-case basis for
potential drug interactions.

- Inability to obtain venous access for sample collection.

- Inability to swallow whole capsules and/or tablets.

- Pregnant female.

- Breastfeeding female.

- The presence of persistent diarrhea or malabsorption that could interfere with the
subject s ability to absorb drugs.

- Illicit drug or alcohol use

- Use of nicotine-containing tobacco products, including cigarettes, vaping and chewing
tobacco.

- Known hypersensitivity to rivaroxaban, apixaban, COBI or DRV.

- History of documented hypersensitivity to sulfa allergy.

- Organ transplant recipient.