Effects of Rifampin on the Pharmacokinetics of Nilotinib in Healthy Subjects

A Phase I Open-label, Two Period, Single Center Study to Assess the Effect of 600 mg Daily Oral Dose of Rifampin (CYP3A4 Inducer) on the Pharmacokinetics of a Single 400 mg Oral Dose of Nilotinib in Healthy Subjects

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT00418756

Enrollment

Registered

2007-01-05

Start date

2006-10-31

Completion date

Unknown

Last updated

2010-03-19

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy

Keywords

nilotinib, Rifampin, PK, healthy subjects

Brief summary

This study will evaluate the effect of 600 mg daily oral dose of rifampin (CYP3A4 inducer) on the pharmacokinetics of a single 400 mg oral dose of nilotinib in healthy subjects

Interventions

DRUGNilotinib

Semi-synthetic antibiotic derivative of rifamycin B and is known to induce cytochrome P-450 (CYP) enzymes.

Study design

Allocation

NON_RANDOMIZED

Intervention model

SINGLE_GROUP

Primary purpose

TREATMENT

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

18 Years to 55 Years

Healthy volunteers

Yes

Inclusion criteria

1. Healthy adult male (18 - 55 yrs) and sterile or post menopausal female subjects: 2. Body weight must be ≥50 kg and \<100 kg, with a body mass index (BMI) \>18 but \<33.

Exclusion criteria

1. Female who is pregnant, test positive for a serum pregnancy test or currently breast feeding. 2. Contraindication to receiving nilotinib or rifampin. 3. Smokers or use of tobacco products or products containing nicotine in the last 30 days 4. A past medical history of clinically significant Electrocardiogram abnormalities, or a history/family history of long QT-interval syndrome. Other protocol-defined inclusion/exclusion may apply.

Design outcomes

Primary

Measure	Time frame
To evaluate the effects of 600 mg rifampin on the pharmacokinetics (PK) of a single 400mg (2 x 200mg capsules) oral dose of AMN107	at pre-dose (0) and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48 and 72 hours post-dose after AMN107 administration on Days 1 and 16.

Secondary

Measure	Time frame
To assess the safety and tolerability of a single 400mg (2x200mg capsules) oral dose of AMN107 given alone and concomitantly with 600mg rifampin	—
To determine the ratio of 6ß - hydroxylcortisol to cortisol in urine as an in-vivomarker of CYP3A4 induction with rifampin treatment4.	on Days -1, 11, 15 and 19

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026