| NCT ID | Title | Phase | Status | Enrollment | Velocity | Design | Start | Completion | Last Updated | Sites | Countries |
|---|---|---|---|---|---|---|---|---|---|---|---|
| NCT02692677 | A Study to Assess the Absorption, Metabolism, and Routes of Excretion Following Oral Administration of (14C) Radiolabeled JNJ--42756493 to Healthy Male Participants | PHASE1 | COMPLETED | 8 | — | — | Mar 1, 2016 | Aug 1, 2016 | Oct 23, 2017 | 1 | United States |
| NCT02218073 | Pharmacokinetic Study of JNJ-42756493 in Healthy Participants | PHASE1 | COMPLETED | 8 | — | — | Oct 1, 2014 | Dec 1, 2014 | Jan 8, 2015 | 1 | Belgium |
| NCT02231489 | Study to Assess the Relative Bioavailability of Orally Administered JNJ-42756493 Tablet Versus JNJ-42756493 Capsule in Healthy Participants | PHASE1 | COMPLETED | 12 | — | — | Sep 1, 2014 | Nov 1, 2014 | Dec 3, 2014 | 1 | Belgium |
The Cmax is the maximum observed plasma concentration.
The Tmax is defined as actual sampling time to reach maximum observed analyte concentration.
The AUC (0-last) is the area under the plasma concentration-time curve from time zero to last quantifiable time.
The AUC (0-infinity) is the area under the plasma concentration-time curve from time zero to infinite time, calculated as the sum of AUC (last) and C(last)/lambda(z); wherein AUC(last) is area under the plasma concentration-time curve from time zero to last quantifiable time, C(last) is the last observed quantifiable concentration, and lambda(z) is elimination rate constant.
Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood.
Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired serum concentration of a drug. Apparent volume of distribution after subcutaneous dose (Vd/F) is influenced by the fraction absorbed.
Lambda(z) is first-order elimination rate constant associated with the terminal portion of the curve, determined as the negative slope of the terminal log-linear phase of the drug concentration-time curve.
The Cmax is the maximum observed plasma concentration.
The AUC (0-infinity) is the area under the plasma concentration-time curve from time zero to infinite time, calculated as the sum of AUC (last) and C(last)/lambda(z); wherein AUC(last) is area under the plasma concentration-time curve from time zero to last quantifiable time, C(last) is the last observed quantifiable concentration, and lambda(z) is elimination rate constant.
The Ae is the amount of drug excreted in urine. It is calculated by multiplying the urinary volume with the urinary drug concentration.
Renal clearance calculated as Ae/AUC (last).
AUMC is defined as the area under first moment plasma concentration-time curve from time of dosing up to definite time t, to infinity, or to the time of last measurable concentration determined by the following equation: AUMC(0 to infinity)=Cntn/k elimination(el) + Cn/k(el\^2) summation\[(tn - tn\^-1) (Cn\^-1) (tn\^-1)\] + Cntn/2 where Cn=last quantifiable concentration, tn=time at which Cn is measured, k=rate constant.
Elimination half-life associated with the terminal slope of the semilogarithmic drug concentration-time curve, calculated as 0.693/Lamda(z).
The Ae%dose is the percentage of drug dose excreted into the urine calculated as (Ae divided by dose)∗100.
Amount of drug excreted into urine over a given time interval from t1 to t2, where t1 and t2 are the start and end times of the interval.
Percentage of the AUCinfinity obtained by extrapolation calculated by ratio between AUCinfinity minus AUClast versus AUCinfinity.
The Cmax is the maximum observed plasma concentration of JNJ-42756493.
Absolute bioavailability will be measured by Area under concentration time-curve (AUC \[0-24\]), AUC (0-last) and AUC (0-infinity).
Relative bioavailability will be measured by AUC (0-24), AUC (0-last) and AUC (0-infinity).
The F (abs) is the percentage of the orally administered dose that is systemically available. It is calculated as (AUC \[0-infinity\] for test)/(AUC \[0-infinity\] for reference \[ref\])\*(D for ref/D for test )\*100, where the reference treatment is an intravenous administration, AUC (0-infinity) is area under the concentration-time curve from time zero to extrapolated infinite time, and D is the dose of orally administered drug.
The F (rel) is the percentage of the orally administered dose that is systemically available. It is calculated as (AUC \[0-infinity\] for test)/(AUC \[0-infinity\] for reference \[ref\])\*(D for test/D for ref )\*100, where the reference treatment is an intravenous administration, AUC (0-infinity) is area under the concentration-time curve from time zero to extrapolated infinite time, and D is the dose of orally administered drug.
| Arm | Type | Description |
|---|---|---|
| JNJ-42756493 | EXPERIMENTAL | Each participant will receive a single oral dose of 12 milligram (mg) of unlabeled JNJ-42756493 admixed with 14C JNJ-42756493 at Pre-dose,0.5,1,2,3,4,8,12 hour post-dose(pd) on Day 1;24,36 h pd on Day 2;48 h pd on Day 3,72 h pd on Day 4; 96 h pd on Day 5;192 h pd on Day 9,216 h pd on Day 10,240 h pd on Day 11,264 h pd on Day 12,288 h pd on Day 13 and 312 h pd on Day 14 |
| Treatment Sequence AB | EXPERIMENTAL | Participants will receive 10 milligram (mg) JNJ-42756493 tablet orally on Day 1 of Period 1 and 100 microgram (mcg) of JNJ-61818549 as intravenous injection 2 hours after the intake of 10 mg JNJ-42756493 oral solution on Day 1 of Period 2. |
| Treatment Sequence BA | EXPERIMENTAL | Participants will receive 100 mcg of JNJ-61818549 as intravenous injection after the intake of 10 mg JNJ-42756493 oral solution on Day 1 of Period 1 and JNJ-42756493 10 mg tablet orally on Day 1 of Period 2. |
| Name | Type | Description |
|---|---|---|
| JNJ-42756493 | DRUG | Participants will receive a single oral solution at a dose of 12 milligram (mg) of unlabeled JNJ--42756493 admixed with 14C- labeled JNJ--42756493. |
| JNJ-42756493 10 mg tablet | DRUG | Participants will be administered with 10 milligram (mg) JNJ-42756493 tablet orally either on Day 1 of Period 1 or on Day 1 of Period 2. |
| JNJ-42756493 10 mg Oral Solution | DRUG | Participants will be administered with 10 mg JNJ-42756493 oral solution either on Day 1 of Period 1 or on Day 1 of Period 2. |
| JNJ-61818549 | DRUG | Participants will receive 100 mcg of JNJ-61818549 as intravenous injection on Day 1 of Period 2 or Day 1 of Period 1. |
| JNJ-42756493 Tablet | DRUG | Participants will receive 10 mg of JNJ-42756493 tablet as single oral dose on Day 1 of each treatment period. |
| JNJ-42756493 Capsule | DRUG | Participants will receive 10 mg of JNJ-42756493 capsule as single oral dose on Day 1 of each treatment period. |
Inclusion Criteria: * Willing to adhere to the prohibitions and restrictions specified in the protocol * A man who is sexually active must agree to use a condom; and a man who is sexually active with a woman of childbearing potential and has not had a vasectomy, must agree to use a condom in combin...