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Selumetinib granule formulation

Phase 1

Neurofibromatosis Type 1 | Small molecule | Other |AstraZeneca PLC|Last Updated: Dec 18, 2025

Success Probability
Approval Probability 71%
TA Base Rate26%
Adjusted LOA41%
ML RiskLOW_RISK
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Market & Valuation
rNPV $3.2B
Market Size $9.4B
Revenue Basis $1.6B
Competitors 6
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Trial Design
UNCONTROLLEDBiomarker
Total Trials1
Total Enrollment36
FDA Designations
No designations recorded
Clinical Trials (1)
NCT IDTitlePhaseStatusEnrollmentVelocityDesignStartCompletionLast UpdatedSitesCountries
NCT05309668Pharmacokinetics, Safety and Efficacy of the Selumetinib Granule Formulation in Children Aged ≥1 to <7 Years With NF1-related Symptomatic, Inoperable PNPHASE1 ACTIVE NOT_RECRUITING 36Jan 21, 2022Apr 28, 2028Dec 18, 202516 United States, Germany +5
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Study Endpoints
Primary Endpoints
Selumetinib AUC0-12 Derived After Single Dose Administration
Pre-dose and 1, 2, 3, 4, 6, 8 and 10-12 hours after selumetinib single dose on the first day of study treatment (Cycle 1 Day 1) (each cycle is 28 days)

To determine the pharmacokinetics of selumetinib after administration of the selumetinib granule formulation

Adverse Events Graded by CTCAE Ver 5.0
from screening until 30 days after last dose

To assess the safety and tolerability of the selumetinib granule formulation.

Secondary Endpoints
Palatability Using the Parent-reported Observer Palatability Questionnaire
Twice daily (morning and evening), from the first day of study treatment (Cycle 1 Day 1) for one week, from Cycle 7 Day 1 for one week (each cycle is 28 days)
Selumetinib and N-desmethyl Selumetinib AUC0-12 Derived After Single and Multiple Dose Administration
Pre-dose and 1, 2, 3, 4, 6, 8, 10-12 and 18-24 hours after selumetinib single dose on the first day of study treatment (Cycle 1 Day 1). Pre-dose, 1, 2, 3, 4, 6, 8, and 10-12 hours post-dose on Cycle 2 Day 1 (each cycle is 28 days)
Selumetinib and N-desmethyl Selumetinib Cmax Derived After Single and Multiple Dose Administration
Pre-dose and 1, 2, 3, 4, 6, 8, 10-12 and 18-24 hours after selumetinib single dose on the first day of study treatment (Cycle 1 Day 1). Pre-dose, 1, 2, 3, 4, 6, 8, and 10-12 hours post-dose on Cycle 2 Day 1 (each cycle is 28 days)
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Study Design & Arms
AllocationNA
MaskingNONE
ModelSINGLE_GROUP
PurposeTREATMENT
Treatment Arms
ArmTypeDescription
Selumetinib single armEXPERIMENTALThis study consists of a screening period (up to 28 days), a treatment period (25 cycles) and a long term safety follow-up for participants until they are 5 years old or commence an alternative systemic NF1-PN treatment, whichever is the earlier. Participants may continue treatment with selumetinib throughout the long term safety follow-up as long as they are considered to be receiving clinical benefit in the opinion of their Investigator. A safety follow up assessment will be performed 30 days after the last dose of study intervention for all study participants.
Interventions
NameTypeDescription
Selumetinib granule formulationDRUGSelumetinib granule formulation will be administered using BSA-based dosing. The granule formulation dose schema to be used in the study will be established in the dose finding phase. At enrolment participants must have a BSA within the range 0.40 to 1.09 m2; once participants attain a BSA between 1.10 and 1.29 m2 they will be encouraged to transition to the capsule formulation, if feasible, although all participants must remain on the granule formulation until after they have completed their third cycle of treatment.
Selumetinib capsule formulationDRUGSelumetinib capsule formulation will be administered using BSA-based dosing. Once participants attain a BSA between 1.10 and 1.29 m2 they will be encouraged to transition to the capsule formulation, if feasible, although all participants must remain on the granule formulation until after they have completed their third cycle of treatment.
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Eligibility Criteria
Age Range1 Year — 6 Years
SexALL
Healthy VolunteersNo
Study Sites16

Inclusion Criteria: 1. Male and female participants aged ≥ 1 to \< 7 years of age at the time their legally authorised representative (parent or guardian) signs the informed consent. 2. All study participants must be diagnosed with NF1 with symptomatic inoperable PN as defined in protocol. 3. Parti...

Countries:United StatesGermanyItalyJapanNetherlandsRussiaSpain
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Recent Changes (Last 90 Days)
LOWMay 26, 2026NCT05309668primaryCompletionDate: changed
LOWMay 24, 2026NCT05309668studyFirstPostDate: changed