Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Also known as Tepotinib
Tepotinib test · 3 trials · 1 indication
The AUC from time zero (= dosing time) extrapolated to infinity, based on the predicted value for the concentration at tlast, as estimated using the linear regression from lambda (λ)z determination.
The AUC from time zero (= dosing time) to time of the last quantifiable concentration (tlast). Calculated using the mixed log-linear trapezoidal rule (linear up, log down).
Cmax was obtained directly from the concentration versus time curve.
Area under the plasma concentration-time curve (AUC) from time zero (= dosing time) to the last sampling time (tlast) at which the concentration is at or above the lower limit of quantification (LLOQ), calculated using the mixed log linear trapezoidal rule (linear up/log down).
Cmax was obtained directly from the concentration versus time curve.
AUC0-t was calculated according to the mixed log linear trapezoidal rule.
AUC0-inf was calculated as AUC0-t + AUCextra. AUCextra represents the extrapolated part of AUC0-inf calculated by Clastcalc/λz, where Clastcalc was the calculated plasma concentration at the last sampling time point at which the measured plasma concentration was at or above the LLOQ and λz was the apparent terminal rate constant determined from the terminal slope of the log-transformed plasma concentration curve.
Cmax was obtained directly from the concentration versus time curve.
Time to reach the maximum plasma concentration (Tmax) was obtained directly from the concentration versus time curve.
| Arm | Type | Description |
|---|---|---|
| Tepotinib then Itraconazole | EXPERIMENTAL | Participants received a single oral dose of Tepotinib 500 milligrams (mg) on Day and Day 12 under fed condition followed by single oral dose of itraconazole 200 mg on Days 8 to 11 and Days 13 to 18. On Day 12, participants received a single dose of 200 mg itraconazole simultaneously with a single dose of 500 mg Tepotinib. |
| Test Treatment then Reference Treatment | EXPERIMENTAL | Participants received a single oral dose of test treatment of tepotinib TF3 (5 \* 100 mg) in treatment period 1 followed by a single oral dose of reference treatment of tepotinib TF3 (2 \* 250 mg) in treatment period 2. The treatment periods were separated by 21 day washout period. |
| Reference Treatment then Test Treatment | EXPERIMENTAL | Participants received a single oral dose of reference treatment of tepotinib TF3 (2 \* 250 mg) in treatment period 1 followed by a single oral dose of test treatment of tepotinib TF3 (5 \* 100 mg) in treatment period 2. The treatment periods were separated by 21 day washout period. |
| First Tepotinib Test, Then Tepotinib Reference | EXPERIMENTAL | - |
| First Tepotinib Reference, Then Tepotinib Test | EXPERIMENTAL | - |
| Name | Type | Description |
|---|---|---|
| Tepotinib (HydroChloride hydrate) | DRUG | Participants received Tepotinib (Hydrochloride hydrate) Film-coated tablet with food on Day 1 and 12 in the morning. |
| Itraconazole | DRUG | Participants received Itraconazole Hard-gelatin capsule with food once daily at the same time in the morning from Day 8 to Day 18; on Day 12 itraconazole is administered concomitantly with tepotinib. |
| Tepotinib 100 mg | DRUG | Participants received a single oral dose of test treatment of tepotinib TF3 (5 \* 100 mg) in either treatment period 1 or 2. |
| Tepotinib 250 mg | DRUG | Participants received a single oral dose of reference treatment of tepotinib TF3 (2 \* 250 mg) in either treatment period 1 or 2. |
| Tepotinib test (Treatment Period 1) | DRUG | Subjects will be administered a single oral dose of test treatment of film-coated tepotinib tablet (1 \* 500 mg tablet) in Treatment period 1 (Day 1) |
| Tepotinib reference (Treatment Period 2) | DRUG | Followed by a 21-day washout after Treatment period 1 (Day 1), subjects will be administered a single oral dose of reference treatment of film-coated tepotinib tablet (5 \* 100 mg tablet) in Treatment period 2 (Day 22) |
| Tepotinib reference (Treatment Period 1) | DRUG | Subjects will be administered a single oral dose of reference treatment of film-coated tepotinib tablet (5 \* 100 mg tablet) in Treatment period 1 (Day 1) |
| Tepotinib test (Treatment Period 2) | DRUG | Followed by a 21-day washout after Treatment period 1 (Day 1), subjects will be administered a single oral dose of test treatment of film-coated tepotinib tablet (1 \* 500 mg tablet) in Treatment period 2 (Day 22) |
Inclusion Criteria: * Overtly healthy participants as determined by medical evaluation, including no clinically significant abnormality identified by medical history, cardiac monitoring, physical examination or laboratory evaluation and no active clinically significant disorder, condition, infectio...
Tepotinib is an investigational small molecule being studied for use in advanced cancer, hepatocellular carcinoma, and non-small cell lung cancer. It is also used in clinical trials involving healthy volunteers to assess drug formulation and interactions. The drug is in Phase 1 clinical development and is not yet approved.
Tepotinib is a kinase inhibitor, as indicated by its '-tinib' suffix, which denotes its target class. It is designed to inhibit specific kinases involved in cancer cell growth and survival. The drug is being evaluated in oncology settings for its potential to treat advanced solid tumors.
Tepotinib is developed by Merck KGaA, a German multinational pharmaceutical company. The company's stock is traded under the ticker MKGAF. Merck KGaA is conducting clinical trials to evaluate the drug's safety and efficacy in various cancer indications.
Tepotinib is currently in Phase 1 clinical development. All completed trials are Phase 1 studies, and there is one active Phase 1 trial ongoing. The drug is investigational and has not received FDA approval for any indication.
Tepotinib has been studied in several Phase 1 trials. Completed trials include NCT03021642, NCT04204902, and NCT05203822, all in healthy volunteers. An active trial, NCT05782361, is studying Tepotinib in combination with pembrolizumab in non-small cell lung cancer.
Tepotinib is the sole name provided for this drug in the available data. No alternative names or aliases have been reported. It is important to refer to the drug by its generic name, Tepotinib, when searching for clinical trial information.