Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
GDC-0973 Infusion · 1 trial · 1 indication
Cmax(dn) is Cmax divided by dose.
AUC (0-t)= Area under the plasma concentration versus time curve from time zero (pre-dose) to time of last quantifiable concentration (0-t).
AUC (0-t)= Area under the plasma concentration versus time curve from time zero (pre-dose) to time of last quantifiable concentration (0-t). AUC (0-t)dn is AUC (0-t) divided by dose.
AUC (0 - ∞)= Area under the plasma concentration versus time curve from time zero (pre-dose) to extrapolated infinite time (0 - ∞). It is obtained from AUC (0 - t) plus AUC (t - ∞).
AUC (0 - ∞)= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞). It is obtained from AUC (0 - t) plus AUC (t - ∞). AUC (0 - ∞)dn is AUC(0 - ∞) divided by dose.
t1/2 is the time measured for the plasma concentration of GDC-0973 to decrease by one half.
CL is a quantitative measure of the rate at which a drug substance is removed from the body.
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. Clearance was estimated from population PK modelling. 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 blood concentration of a drug. Vss is the apparent volume of distribution at steady-state.
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 plasma concentration of a drug. Vz/F is influenced by the fraction absorbed.
Absolute oral bioavailability is the amount of drug from a formulation that reaches the systemic circulation relative to an IV dose. F = \[AUC (0-∞), oral multiplied by Dose IV\] divided by \[AUC (0-∞), IV multiplied by Dose oral\]. Absolute oral bioavailability is determined for drugs which are administered orally. IV dose is 100% in systemic circulation (dosed directly) and hence no estimation is required.
MAT is mean time required for the drug to reach the central compartment. MAT was estimated from the mean resident time (MRT) from oral and IV administration. MAT was calculated as MRT last of oral dose minus MRT last of IV dose. MAT is analyzed when drug is administered orally (only for non-IV routes of administration).
The cumulative amount of drug excreted in urine over the entire collection interval of 96 hrs was calculated by adding the Aeu of the intervals 0 to 12, 12 to 24, 24 to 48, 48 to 72, and 72 to 96 hrs where Aeu was calculated by multiplying the urine volume within the collection interval by the associated drug concentration.
CLR was calculated as Aeu divided by AUC (0 - ∞), where Aeu was amount of drug excreted in urine from time 0 to 96 hrs post-dose and AUC(0 - ∞) was area under the concentration-time curve of the analyte in plasma over the time interval from zero extrapolated to infinity hrs post-dose.
% Excreted is the mean percentage of dose recovery in urine and calculated as: (Aeu divided by dose) multiplied by 100, where Aeu was amount of drug excreted in urine from time 0 to 96 hrs post-dose.
| Arm | Type | Description |
|---|---|---|
| Part 1: GDC-0973 IV Infusion First, Then GDC-0973 Capsules | EXPERIMENTAL | Participants will receive single dose of GDC-0973 2 milligrams (mg) IV infusion in first intervention period followed by single dose of GDC-0973 20 mg oral capsules (four 5-mg capsules) in second intervention period. The washout period between each period will be a minimum of 10 days. |
| Part 2: GDC-0973 IV Infusion First, Then GDC-0973 Capsules | EXPERIMENTAL | Participants will receive single dose of GDC-0973 2 mg IV infusion in first intervention period followed by single dose of GDC-0973 20 mg oral capsules (four 5-mg capsules) in second intervention period. The washout period between each period will be a minimum of 10 days. |
| Part 2: GDC-0973 Capsules First, Then GDC-0973 IV Infusion | EXPERIMENTAL | Participants will receive single dose of GDC-0973 20 mg oral capsules (four 5-mg capsules) in first intervention period followed by single dose of GDC-0973 2 mg IV infusion in second intervention period. The washout period between each period will be a minimum of 10 days. |
| Name | Type | Description |
|---|---|---|
| GDC-0973 IV Infusion | DRUG | IV infusion. |
| GDC-0973 Oral Capsules | DRUG | Oral dose. |
Inclusion Criteria * Within body mass index range 18.5 to 29.9 kilograms per square meter (kg/m\^2) * In good health, determined by no clinically significant findings from medical history, 12-lead electrocardiogram (ECG), and vital signs * Clinical laboratory evaluations within the reference range ...
GDC-0973 Infusion is a small molecule being studied in healthy volunteers to assess its absolute bioavailability. It is administered intravenously and compared to oral administration of GDC-0973 (cobimetinib) in a Phase 1 clinical trial. The drug is investigational and not yet approved for any condition.
GDC-0973 Infusion is developed by Roche Holding AG, traded on the OTC market under the ticker RHHBY. The company is conducting clinical research on this investigational small molecule drug.
GDC-0973 Infusion is in Phase 1 clinical development. It is an investigational drug, meaning it has not been approved by regulatory authorities. The Phase 1 trial has been completed.
GDC-0973 Infusion was studied in one completed Phase 1 trial, NCT01249118, titled "An Absolute Bioavailability Study in Healthy Participants Comparing Oral to Intravenous Administration of GDC-0973 (Cobimetinib)." The trial enrolled 13 healthy volunteers aged 18 years and older.
GDC-0973 Infusion is the intravenous form of GDC-0973, which is also known as cobimetinib. The clinical trial compares oral administration of GDC-0973 (cobimetinib) to intravenous administration of GDC-0973 Infusion to measure absolute bioavailability.