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Trametinib

Phase 1

Cancer | Small molecule | Oncology |Novartis AG|Last Updated: Feb 9, 2022

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Trial Design
CONTROLLED
Total Trials1
Total Enrollment139
FDA Designations
No designations recorded
Clinical trial landscape

Trametinib · 2 trials · 2 indications

Phase 1 2
NCT02705963A Drug-Drug Interaction Study to Assess the Effect of Trametinib on the Pharmacokinetics of an Oral Contraceptive in Female Patients With Solid TumorsSolid Tumors
COMPLETED19 Analytics
NCT02124772Study to Investigate Safety, Pharmacokinetic (PK), Pharmacodynamic (PD) and Clinical Activity of Trametinib in Subjects With Cancer or Plexiform Neurofibromas and Trametinib in Combination With Dabrafenib in Subjects With Cancers Harboring V600 MutationsCancer
COMPLETED139 Analytics
PHASE1COMPLETED
A Drug-Drug Interaction Study to Assess the Effect of Trametinib on the Pharmacokinetics of an Oral Contraceptive in Female Patients With Solid Tumors
Solid TumorsUnlock trial analytics
PHASE1COMPLETED
Study to Investigate Safety, Pharmacokinetic (PK), Pharmacodynamic (PD) and Clinical Activity of Trametinib in Subjects With Cancer or Plexiform Neurofibromas and Trametinib in Combination With Dabrafenib in Subjects With Cancers Harboring V600 Mutations
CancerUnlock trial analytics
Study Endpoints
Primary Endpoints
Pharmacokinetics parameter: AUCtau of NE and EE alone and in combination with trametinib
Day 5 and 6 and 21 and 22

To evaluate the effect of multiple doses of trametinib (2 mg once daily) on the steady state pharmacokinetics of combination OC (NE and EE) in female patients with solid tumors.

Pharmacokinetics parameter: AUClast of NE and EE alone and in combination with trametinib
Day 5 and 6 and 21 and 22

To evaluate the effect of multiple doses of trametinib (2 mg once daily) on the steady state pharmacokinetics of combination OC (NE and EE) in female patients with solid tumors.

Pharmacokinetics parameter: Cmax of NE and EE alone and in combination with trametinib
Day 5 and 6 and 21 and 22

To evaluate the effect of multiple doses of trametinib (2 mg once daily) on the steady state pharmacokinetics of combination OC (NE and EE) in female patients with solid tumors.

Pharmacokinetics parameter: Tmax of NE and EE alone and incombination with trametinib
Days 5 and 6 and 21 and 22

To evaluate the effect of multiple doses of trametinib (2 mg once daily) on the steady state pharmacokinetics of combination OC (NE and EE) in female patients with solid tumors.

Incidence of Treatment Emergent Adverse Events in Subjects Treated With Trametinib Monotherapy
From the day of the first dose of trametinib up to 30 days after the last dose, up to maximum duration of 64 months

Incidence of treatment emergent adverse events is defined as number of participants with adverse events (AEs) and serious adverse events (SAEs), including changes from baseline in vital signs and laboratory results qualifying and reported as AEs. The number of participants in each category is reported in the table.

Average Steady State Plasma Concentration (Cavg) of Trametinib When Administered Alone (Monotherapy)
pre dose, 1, 2, 4, 7, 10 and 24 hours post trametinib dose on Cycle 1 Day 15. The duration of 1 cycle was 28 days.

Pharmacokinetic (PK) parameters were calculated based on trametinib plasma concentrations by using non-compartmental methods. The average steady state plasma concentration (Cavg) of trametinib was calculated as the ratio of area under the curve (AUC)/tau, where tau = 24 h for trametinib.

Secondary Endpoints
Pharmacokinetics parameter: AUClast of M5
Day 21 and 22
Pharmacokinetics parameter: AUCtau of M5
Day 21 and 22
Pharmacokinetics parameter: Cmax of M5
Day 21 and 22
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Study Design & Arms
AllocationNA
MaskingNONE
ModelSINGLE_GROUP
PurposeTREATMENT
Treatment Arms
ArmTypeDescription
Oral Contraceptive / TrametinibEXPERIMENTALIn treatment period 1 of the PK Phase patients will take the Oral Contraceptive once daily from Days 1-5. Period 2 of the PK Phase starts on Day 6 when patients take both the Oral Contraceptive and trametinib once daily from Days 6 to 21. Patients may continue dosing with trametinib only once daily from Day 22 onwards (post PK Phase).
Part A - TMT 0.0125 mg/kg/dayEXPERIMENTALParticipants treated with trametinib 0.0125 mg/kg/day
Part A - TMT 0.025 mg/kg/dayEXPERIMENTALParticipants treated with trametinib 0.025 mg/kg/day
Part A - TMT 0.032 mg/kg/dayEXPERIMENTALParticipants under 6 years of age treated with trametinib 0.032 mg/kg/day
Part A - TMT 0.04 mg/kg/dayEXPERIMENTALParticipants treated with trametinib 0.04 mg/kg/day
Part B - NeuroblastomaEXPERIMENTALParticipants with refractory or relapsed neuroblastoma treated with trametinib 0.025 mg/kg/day
Part B - LGG fusionEXPERIMENTALParticipants with refractory or relapsed neuroblastoma treated with trametinib 0.025 mg/kg/day
Part B - NF-1 with PNEXPERIMENTALParticipants with neurofibromatosis Type -1 associated plexiform neurofibromas (NF-1 with PN) treated with trametinib 0.025 mg/kg/day
Part B - BRAF V600 mutant solid tumorEXPERIMENTALParticipants with BRAF V600 mutant solid tumors treated with trametinib 0.025 mg/kg/day
Part C - TMT 0.025 mg/kg/day + 50% DRB RP2DEXPERIMENTALParticipants treated with a combination therapy of trametinib (0.025 mg/kg/day) plus 50% of the recommended phase II dose (RP2D) of dabrafenib monotherapy (2.63 mg/kg/day for \<12 years old subjects and 2.25 mg/kg/day for ≥12 years old subjects)
Part C - TMT 0.025 mg/kg/day + 100% DRB RP2DEXPERIMENTALParticipants treated with a combination therapy of trametinib (0.025 mg/kg/day) plus 100% of the recommended phase II dose (RP2D) of dabrafenib monotherapy (5.25 mg/kg/day for \<12 years old subjects and 4.5 mg/kg/day for ≥12 years old subjects)
Part C - TMT 0.032 mg/kg/day + 100% DRB RP2DEXPERIMENTALParticipants under 6 years of age treated with a combination therapy of trametinib (0.032 mg/kg/day) with 100% of the recommended phase II dose (RP2D) of dabrafenib monotherapy (5.25 mg/kg/day)
Part D - LGGEXPERIMENTALParticipants with low grade glioma (LGG) treated with a combination therapy of trametinib (0.032 mg/kg/day for \< 6 years old subjects and 0.025 mg/kg/day for ≥ 6 years old subjects) plus 100% of the recommended phase II dose (RP2D) of dabrafenib monotherapy (5.25 mg/kg/day for \<12 years old subjects and 4.5 mg/kg/day for ≥12 years old subjects)
Part D - LCHEXPERIMENTALParticipants with Langerhans cell histiocytosis (LCH) treated with a combination therapy of trametinib (0.032 mg/kg/day for \< 6 years old subjects and 0.025 mg/kg/day for ≥ 6 years old subjects) plus 100% of the recommended phase II dose (RP2D) of dabrafenib monotherapy (5.25 mg/kg/day for \<12 years old subjects and 4.5 mg/kg/day for ≥12 years old subjects)
Interventions
NameTypeDescription
TrametinibDRUGEach tablet is 2mg trametinib to be taken orally once daily.
Oral Contraceptive (1mg norethindrone, 0.035mg ethinyl estradiol)DRUGCombined oral contraceptive to be taken orally once daily.
DabrafenibDRUGDabrafenib was administered orally, twice daily. The daily dose was divided into two equal doses. It was available in capsules (50 mg and 75 mg), dispersible tablets (10 mg) and powder for oral suspension (10 mg/mL dose).
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Eligibility Criteria
Age Range18 Years to 59 Years
SexFEMALE
Healthy VolunteersNo
Study Sites7

Inclusion Criteria: * Has a histologically or cytologically confirmed diagnosis of a solid tumor malignancy (except for any excluded malignancies listed in the Exclusion Criteria) that is not responsive to standard therapy(ies) or for which there is no approved therapy. * Meets one of the following...

Countries:United StatesBelgiumNetherlandsSpainUnited KingdomAustraliaCanadaFrance
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