Trial Outcomes & Findings for Influence of Rifampin on the Pharmacokinetics of Romidepsin in Patients With Advanced Cancer (NCT NCT01324323)

NCT ID: NCT01324323

Last Updated: 2019-11-25

Results Overview

AUC0-t: area under the plasma concentration time-curve from Time 0 to the time of the last quantifiable concentration (Ct), calculated by linear trapezoidal method when concentrations are increasing and the logarithmic trapezoidal method when concentrations are decreasing.

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

14 participants

Primary outcome timeframe

Days 1 and 8; at 0 (pre-dose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Results posted on

2019-11-25

Participant Flow

The study was conducted at 3 study centers (2 in the United States and 1 in the United Kingdom). The first subject was enrolled in April 2011 and the last subject completed the study in Feb 2012.

Participant milestones

Participant milestones
Measure
Romidepsin and Rifampin
Romidepsin 14 mg/m\^2 intravenous infused over 4 hours on Day 1 and Day 8. Rifampin 600 mg oral once daily on Days 4-8
Overall Study
STARTED
14
Overall Study
COMPLETED
13
Overall Study
NOT COMPLETED
1

Reasons for withdrawal

Reasons for withdrawal
Measure
Romidepsin and Rifampin
Romidepsin 14 mg/m\^2 intravenous infused over 4 hours on Day 1 and Day 8. Rifampin 600 mg oral once daily on Days 4-8
Overall Study
Withdrawal by Subject
1

Baseline Characteristics

Influence of Rifampin on the Pharmacokinetics of Romidepsin in Patients With Advanced Cancer

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure
Romidepsin and Rifampin
n=14 Participants
Romidepsin 14 mg/m\^2 intravenous infused over 4 hours on Day 1 and Day 8. Rifampin 600 mg oral once daily on Days 4-8
Age, Continuous
63.6 years
STANDARD_DEVIATION 12.57 • n=93 Participants
Sex: Female, Male
Female
9 Participants
n=93 Participants
Sex: Female, Male
Male
5 Participants
n=93 Participants
Race/Ethnicity, Customized
White
13 Participants
n=93 Participants
Race/Ethnicity, Customized
Black or African American
1 Participants
n=93 Participants
Race/Ethnicity, Customized
Other
0 Participants
n=93 Participants
Race/Ethnicity, Customized
Hispanic or Latino
0 Participants
n=93 Participants
Race/Ethnicity, Customized
Not Hispanic or Latino
14 Participants
n=93 Participants
Race/Ethnicity, Customized
Unknown or Not Reported
0 Participants
n=93 Participants
Region of Enrollment
United Kingdom
5 participants
n=93 Participants
Region of Enrollment
United States
9 participants
n=93 Participants
Height
167.6 Centimeters
STANDARD_DEVIATION 9.54 • n=93 Participants
Weight
78.2 kilograms
STANDARD_DEVIATION 18.85 • n=93 Participants
Body Surface Area (BSA)
1.9 Metered Squares m^2
STANDARD_DEVIATION 0.22 • n=93 Participants
Eastern Cooperative Oncology Group Performance Status (ECOG)
0 = Fully active
7 Participants
n=93 Participants
Eastern Cooperative Oncology Group Performance Status (ECOG)
1 = Restricted in physical strenuous activity
7 Participants
n=93 Participants
Eastern Cooperative Oncology Group Performance Status (ECOG)
2 = Ambulaotry but unable to work
0 Participants
n=93 Participants
Eastern Cooperative Oncology Group Performance Status (ECOG)
3 = Limited Self-Care
0 Participants
n=93 Participants
Eastern Cooperative Oncology Group Performance Status (ECOG)
4 = Completely Disabled
0 Participants
n=93 Participants

PRIMARY outcome

Timeframe: Days 1 and 8; at 0 (pre-dose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Population: The PK population included all participants who received at least 1 dose of study drug and had evaluable PK profiles. The primary reason for study discontinuation for the 1 participant was due to withdrawal of consent.

AUC0-t: area under the plasma concentration time-curve from Time 0 to the time of the last quantifiable concentration (Ct), calculated by linear trapezoidal method when concentrations are increasing and the logarithmic trapezoidal method when concentrations are decreasing.

Outcome measures

Outcome measures
Measure
Romidepsin Day 1
n=14 Participants
Romidepsin 14 mg/m\^2 intravenous infused over 4 hours on Day 1 and Day 8.
Romidepsin and Rifampin Day 8
n=13 Participants
Romidepsin 14mg/m\^2 intravenous infused over 4 hours on Day 8. Rifampin 600mg oral once daily on Days 4-8.
Area Under the Plasma Concentration Time-curve From Time 0 to the Time of the Last Quantifiable Concentration (AUC0-t)of Romidepsin
2225.1 ng*hr/mL
Geometric Coefficient of Variation 71.4
3966.3 ng*hr/mL
Geometric Coefficient of Variation 76.5

PRIMARY outcome

Timeframe: Day 1 and Day 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Population: The PK population included all participants who received at least 1 dose of study drug and had evaluable PK profiles. The primary reason for study discontinuation for the 1 participant was due to withdrawal of consent.

Individual and mean romidepsin plasma concentrations by treatment and scheduled time data were collected. AUC0-24: area under the plasma concentration time-curve from Time 0 to 24 hours, calculated by linear trapezoidal method when concentrations are increasing and the logarithmic trapezoidal method when concentrations are decreasing.

Outcome measures

Outcome measures
Measure
Romidepsin Day 1
n=14 Participants
Romidepsin 14 mg/m\^2 intravenous infused over 4 hours on Day 1 and Day 8.
Romidepsin and Rifampin Day 8
n=13 Participants
Romidepsin 14mg/m\^2 intravenous infused over 4 hours on Day 8. Rifampin 600mg oral once daily on Days 4-8.
Area Under the Plasma Concentration Time-curve From Time 0 to 24-hour (AUC0-24) for Romidepsin
2204.2 ng*hr/mL
Geometric Coefficient of Variation 72.0
3903.9 ng*hr/mL
Geometric Coefficient of Variation 78.0

PRIMARY outcome

Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Population: The primary objective was to assess the influence of multiple doses of rifampin on the PK of romidepsin. The PK population included all participants who received at least 1 dose of study drug and had evaluable PK profiles. The primary reason for study discontinuation for the 1 participant was due to withdrawal of consent.

AUC0-∞: area under the plasma concentration time-curve from Time 0 extrapolated to infinity, calculated as \[AUCt + Ct/λz\]. λz is the apparent terminal rate constant. No AUC extrapolation was performed with unreliable λz. If the percentage of AUC extrapolated is ≥ 25%, AUC0-∞ will not be reported.

Outcome measures

Outcome measures
Measure
Romidepsin Day 1
n=14 Participants
Romidepsin 14 mg/m\^2 intravenous infused over 4 hours on Day 1 and Day 8.
Romidepsin and Rifampin Day 8
n=13 Participants
Romidepsin 14mg/m\^2 intravenous infused over 4 hours on Day 8. Rifampin 600mg oral once daily on Days 4-8.
Area Under the Plasma Concentration Time-curve From Time Zero Extrapolated to Infinity (AUC0-∞).
2229.8 ng*hr/mL
Geometric Coefficient of Variation 71.3
3980.7 ng*hr/mL
Geometric Coefficient of Variation 76.1

PRIMARY outcome

Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Population: The primary objective was to assess the influence of multiple doses of rifampin on the PK of romidepsin. The PK population included all participants who received at least 1 dose of study drug and had evaluable PK profiles. The primary reason for study discontinuation for the 1 participant was due to withdrawal of consent.

Maximum observed plasma concentration (Cmax)was obtained directly from the observed concentration versus time data.

Outcome measures

Outcome measures
Measure
Romidepsin Day 1
n=14 Participants
Romidepsin 14 mg/m\^2 intravenous infused over 4 hours on Day 1 and Day 8.
Romidepsin and Rifampin Day 8
n=13 Participants
Romidepsin 14mg/m\^2 intravenous infused over 4 hours on Day 8. Rifampin 600mg oral once daily on Days 4-8.
Maximum Observed Plasma Concentration (Cmax)of Romidepsin
571.2 ng/mL
Geometric Coefficient of Variation 81.0
900.1 ng/mL
Geometric Coefficient of Variation 104.9

PRIMARY outcome

Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Population: The primary objective was to assess the influence of multiple doses of rifampin on the PK of romidepsin. The PK population included all participants who received at least 1 dose of study drug and had evaluable PK profiles. The primary reason for study discontinuation for the 1 participant was due to withdrawal of consent.

Time to maximum observed plasma concentration (Tmax) was obtained directly from the observed concentration versus time data.

Outcome measures

Outcome measures
Measure
Romidepsin Day 1
n=14 Participants
Romidepsin 14 mg/m\^2 intravenous infused over 4 hours on Day 1 and Day 8.
Romidepsin and Rifampin Day 8
n=13 Participants
Romidepsin 14mg/m\^2 intravenous infused over 4 hours on Day 8. Rifampin 600mg oral once daily on Days 4-8.
Time to Maximum Observed Plasma Concentration (Tmax)
3.0 hours
Full Range 51.5 • Interval 1.0 to 5.0
3.00 hours
Full Range 50.7 • Interval 1.0 to 4.27

PRIMARY outcome

Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Population: The primary objective was to assess the influence of multiple doses of rifampin on the PK of romidepsin. The PK population included all participants who received at least 1 dose of study drug and had evaluable PK profiles. The primary reason for study discontinuation for the 1 participant was due to withdrawal of consent.

The terminal elimination half-life (t1/2) in plasma, was calculated as \[(ln 2)/λz\]. This was only calculated when a reliable estimate for λz could be obtained.

Outcome measures

Outcome measures
Measure
Romidepsin Day 1
n=14 Participants
Romidepsin 14 mg/m\^2 intravenous infused over 4 hours on Day 1 and Day 8.
Romidepsin and Rifampin Day 8
n=13 Participants
Romidepsin 14mg/m\^2 intravenous infused over 4 hours on Day 8. Rifampin 600mg oral once daily on Days 4-8.
Estimate of the Terminal Elimination Half-life in Plasma (t1/2)
9.666 hours
Geometric Coefficient of Variation 27.9
8.341 hours
Geometric Coefficient of Variation 24.0

PRIMARY outcome

Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Population: The primary objective was to assess the influence of multiple doses of rifampin on the PK of romidepsin. The PK population included all participants who received at least 1 dose of study drug and had evaluable PK profiles. The primary reason for study discontinuation for the 1 participant was due to withdrawal of consent.

The apparent total plasma clearance (CL) was calculated as \[Dose/AUC0-∞\] for Romidepsin alone and co-administered with rifampin plasma concentrations.

Outcome measures

Outcome measures
Measure
Romidepsin Day 1
n=14 Participants
Romidepsin 14 mg/m\^2 intravenous infused over 4 hours on Day 1 and Day 8.
Romidepsin and Rifampin Day 8
n=13 Participants
Romidepsin 14mg/m\^2 intravenous infused over 4 hours on Day 8. Rifampin 600mg oral once daily on Days 4-8.
Clearance (CL): Apparent Total Plasma Clearance.
11.59 L/hr
Geometric Coefficient of Variation 78.1
6.45 L/hr
Geometric Coefficient of Variation 82.2

PRIMARY outcome

Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Population: The PK population was to consist of all participants who received at least 1 dose of study drug and had evaluable PK profiles.

Apparent total volume of distribution (Vz) was calculated as \[(CL)/λz\] for Romidepsin and co-administered with Rifampin.

Outcome measures

Outcome measures
Measure
Romidepsin Day 1
n=14 Participants
Romidepsin 14 mg/m\^2 intravenous infused over 4 hours on Day 1 and Day 8.
Romidepsin and Rifampin Day 8
n=13 Participants
Romidepsin 14mg/m\^2 intravenous infused over 4 hours on Day 8. Rifampin 600mg oral once daily on Days 4-8.
Apparent Total Volume of Distribution (Vz).
161.48 Liters
Geometric Coefficient of Variation 78.6
77.6 Liters
Geometric Coefficient of Variation 93.8

SECONDARY outcome

Timeframe: Day 1 up to Day 36 (28 days after the last treatment)

Population: The safety population included all subjects who received at least 1 dose of study drug.

AEs were considered related if assessed by the Investigator as possibly, probably or definitely related to study drug. Serious AEs (SAEs) are those that resulted in death, were life-threatening, required or prolonged inpatient hospitalization, resulted in persistent or significant disability/incapacity, congenital anomaly, or resulted in an important medical event that may have jeopardized the patient or required medical or surgical intervention to prevent one of the outcomes listed above.

Outcome measures

Outcome measures
Measure
Romidepsin Day 1
n=14 Participants
Romidepsin 14 mg/m\^2 intravenous infused over 4 hours on Day 1 and Day 8.
Romidepsin and Rifampin Day 8
Romidepsin 14mg/m\^2 intravenous infused over 4 hours on Day 8. Rifampin 600mg oral once daily on Days 4-8.
Summary of Participants With Treatment Emergent Adverse Events (TEAEs)
= > 1 TEAE related to any study drug
13 participants
Summary of Participants With Treatment Emergent Adverse Events (TEAEs)
= > 1 TEAE leading to discontinuation
0 participants
Summary of Participants With Treatment Emergent Adverse Events (TEAEs)
= > 1 TEAE related discontinuation to any drug
0 participants
Summary of Participants With Treatment Emergent Adverse Events (TEAEs)
= > 1 Romidepsin related TEAE discontinuation
0 participants
Summary of Participants With Treatment Emergent Adverse Events (TEAEs)
= > 1 TEAE related to Romidepsin
13 participants
Summary of Participants With Treatment Emergent Adverse Events (TEAEs)
= > 1 Rifampin related TEAE discontinuation
0 participants
Summary of Participants With Treatment Emergent Adverse Events (TEAEs)
= > 1 TEAE related to Rifampin
2 participants
Summary of Participants With Treatment Emergent Adverse Events (TEAEs)
= > 1 Serious TEAE
2 participants
Summary of Participants With Treatment Emergent Adverse Events (TEAEs)
= > 1 Serious TEAE related to any drug
1 participants
Summary of Participants With Treatment Emergent Adverse Events (TEAEs)
= > 1 Serious TEAE related to Romidepsin
1 participants
Summary of Participants With Treatment Emergent Adverse Events (TEAEs)
= > 1 Serious TEAE related to Rifampin
1 participants
Summary of Participants With Treatment Emergent Adverse Events (TEAEs)
= > 1 TEAE
13 participants
Summary of Participants With Treatment Emergent Adverse Events (TEAEs)
Participants who died
0 participants

Adverse Events

Romidepsin Plus Rifampin

Serious events: 2 serious events
Other events: 13 other events
Deaths: 0 deaths

Serious adverse events

Serious adverse events
Measure
Romidepsin Plus Rifampin
n=14 participants at risk
Romidepsin 14 mg/m\^2 intravenous infused over 4 hours on Day 1 and Day 8 and Rifampin 600 mg oral once daily on Days 4-8.
Blood and lymphatic system disorders
Anaemia
14.3%
2/14 • Day 1 up to Day 36 (28 days after last treatment)
Gastrointestinal disorders
Vomiting
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
General disorders
Fatigue
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
Gastrointestinal disorders
Nausea
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
Blood and lymphatic system disorders
Thrombocytopenia
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
Gastrointestinal disorders
Melaena
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)

Other adverse events

Other adverse events
Measure
Romidepsin Plus Rifampin
n=14 participants at risk
Romidepsin 14 mg/m\^2 intravenous infused over 4 hours on Day 1 and Day 8 and Rifampin 600 mg oral once daily on Days 4-8.
Gastrointestinal disorders
Nausea
71.4%
10/14 • Day 1 up to Day 36 (28 days after last treatment)
Gastrointestinal disorders
Vomiting
42.9%
6/14 • Day 1 up to Day 36 (28 days after last treatment)
Gastrointestinal disorders
Diarrhoea
35.7%
5/14 • Day 1 up to Day 36 (28 days after last treatment)
Gastrointestinal disorders
Constipation
14.3%
2/14 • Day 1 up to Day 36 (28 days after last treatment)
Gastrointestinal disorders
Abdominal Pain
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
Gastrointestinal disorders
Abdominal Pain Upper
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
Gastrointestinal disorders
Flatulence
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
Gastrointestinal disorders
Gastrooesophageal Reflux Disease
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
General disorders
Fatigue
42.9%
6/14 • Day 1 up to Day 36 (28 days after last treatment)
General disorders
Asthenia
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
General disorders
Malaise
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
General disorders
Non-Cardiac Chest Pain
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
Blood and lymphatic system disorders
Thrombocytopenia
35.7%
5/14 • Day 1 up to Day 36 (28 days after last treatment)
Blood and lymphatic system disorders
Anaemia
21.4%
3/14 • Day 1 up to Day 36 (28 days after last treatment)
Metabolism and nutrition disorders
Decreased Appetite
42.9%
6/14 • Day 1 up to Day 36 (28 days after last treatment)
Metabolism and nutrition disorders
Hypokalaemia
14.3%
2/14 • Day 1 up to Day 36 (28 days after last treatment)
Musculoskeletal and connective tissue disorders
Arthralgia
14.3%
2/14 • Day 1 up to Day 36 (28 days after last treatment)
Musculoskeletal and connective tissue disorders
Musculoskeletal Discomfort
14.3%
2/14 • Day 1 up to Day 36 (28 days after last treatment)
Musculoskeletal and connective tissue disorders
Musculoskeletal Pain
14.3%
2/14 • Day 1 up to Day 36 (28 days after last treatment)
Musculoskeletal and connective tissue disorders
Back Pain
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
Musculoskeletal and connective tissue disorders
Musculoskeletal Chest Pain
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
Nervous system disorders
Dysgeusia
14.3%
2/14 • Day 1 up to Day 36 (28 days after last treatment)
Nervous system disorders
Dizziness
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
Nervous system disorders
Lethargy
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
Psychiatric disorders
Anxiety
21.4%
3/14 • Day 1 up to Day 36 (28 days after last treatment)
Psychiatric disorders
Insomnia
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
Respiratory, thoracic and mediastinal disorders
Cough
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
Respiratory, thoracic and mediastinal disorders
Dyspnoea
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
Respiratory, thoracic and mediastinal disorders
Oropharyngeal Pain
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
Skin and subcutaneous tissue disorders
Decubitus Ulcer
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)
Gastrointestinal disorders
Haemorrhoids
7.1%
1/14 • Day 1 up to Day 36 (28 days after last treatment)

Additional Information

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Celgene Corporation

Phone: 1-888-260-1599

Results disclosure agreements

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