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pralsetinib

Phase 1

RET-altered Non Small Cell Lung Cancer | Small molecule | Oncology |Roche Holding AG|Last Updated: May 31, 2025

Target and mechanism

Molecular targetRET, CCDC6, KIF5B
Target classInhibitor
ModalitySmall molecule

Success Probability

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Market & Valuation

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Trial Design

CONTROLLEDDMC
Total Trials1
Total Enrollment590

FDA Designations

No designations recorded

Clinical trial landscape

pralsetinib · 1 trial · 40 indications

Phase 1 1
NCT03037385Phase 1/2 Study of the Highly-selective RET Inhibitor, Pralsetinib (BLU-667), in Participants With Thyroid Cancer, Non-Small Cell Lung Cancer, and Other Advanced Solid TumorsRET-altered Non Small Cell Lung Cancer
COMPLETED590 Analytics
PHASE1COMPLETED
Phase 1/2 Study of the Highly-selective RET Inhibitor, Pralsetinib (BLU-667), in Participants With Thyroid Cancer, Non-Small Cell Lung Cancer, and Other Advanced Solid Tumors
RET-altered Non Small Cell Lung CancerUnlock trial analytics

Study Endpoints

Primary Endpoints

Phase 1 : Maximum Tolerated Dose (MTD) and Recommended Phase 2 Dose (RP2D) of Pralsetinib
Up to approximately 30.8 months

MTD was defined as the highest tolerated dose of pralsetinib without causing dose limiting toxicities (DLTs). DLT was defined as any Grade ≥3 adverse event (AE) occurring during Cycle 1 during Phase 1 (dose escalation) that is not clearly caused by something other than pralsetinib. RP2D was defined as the highest dose with acceptable toxicity as determined from dose-escalation phase.

Phase 1 and Phase 2: Number of Participants With AEs and Serious AEs (SAEs)
From Cycle 1 Day 1 up to 30 days after the final dose of study drug (up to approximately 6.7 years)

An AE was any untoward medical occurrence associated with the use of a drug in humans, whether or not considered drug related. An AE can be any unfavorable and unintended sign (e.g., an abnormal laboratory finding), symptom, or disease temporally associated with the use of a drug, without any judgment about causality. A SAE is any significant hazard, contraindication, side effect that is fatal or life-threatening, requires hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly or birth defect, is medically significant or requires intervention to prevent one or other of the outcomes listed above.

Phase 2: Overall Response Rate (ORR)
Up to approximately 79.8 months

ORR was defined as the percentage of participants with a confirmed complete response (CR) or partial response (PR) for at least two assessments with at least 28 days apart and no disease progression (PD) in between. Per Response Evaluation Criteria in Solid Tumors, Version 1.1 (RECIST v1.1), CR was defined as the disappearance of all target lesions or any pathological lymph nodes (whether target or non-target) having a reduction in the short axis to \<10 millimeters (mm). PR was defined as at least a 30% decrease in the sum of diameters (SOD) of all target lesions, taking as reference the baseline SOD, in the absence of CR. PD was defined as at least a 20% increase in SOD of target lesions, taking as reference the smallest SOD on study (including baseline). ORR and its two-sided 95% CI, based on the exact binomial distribution (Clopper-Pearson), were presented.

Secondary Endpoints

Phase 1: ORR
Up to approximately 28 months
Phase 1 and Phase 2: ORR in RET-fusion Positive NSCLC Participants With Specific RET Gene Status
Up to approximately 79.8 months
Phase 1 and Phase 2: ORR in RET-mutation MTC Participants With Specific RET Gene Status
Up to approximately 79.8 months
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Study Design & Arms

AllocationNON_RANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Phase 1 Dose EscalationEXPERIMENTALMultiple doses of pralsetinib (BLU-667) for oral administration.
Phase 2 Dose ExpansionEXPERIMENTALOral dose of pralsetinib (BLU-667) as determined during Dose Escalation.

Interventions

NameTypeDescription
pralsetinib (BLU-667)DRUGpralsetinib (BLU-667) is a potent and selective inhibitor of the RET mutations, fusions, and predicted resistant mutants
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites71

Key Inclusion Criteria: * Diagnosis during dose escalation (Phase 1) - Pathologically documented, definitively diagnosed non-resectable advanced solid tumor. * All participants treated at doses \> 120 mg per day must have MTC, or a RET-altered solid tumor per local assessment of tumor tissue and...

Countries:United StatesBelgiumChinaFranceGermanyHong KongItalyNetherlandsSingaporeSouth KoreaSpainTaiwanUnited Kingdom
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Frequently asked questions about pralsetinib

What is pralsetinib used for in RET-altered Non Small Cell Lung Cancer?

Pralsetinib is an investigational small molecule being studied for the treatment of RET-altered Non Small Cell Lung Cancer. It is also being evaluated in other RET-altered solid tumors, including thyroid cancer, colon cancer, and medullary thyroid cancer. The drug is currently in Phase 1 clinical development.

What does pralsetinib target?

Pralsetinib targets RET, a receptor tyrosine kinase. It is a highly-selective RET inhibitor, designed to block the activity of RET fusion proteins and mutations that drive tumor growth. This makes it a targeted therapy for cancers with RET alterations, such as RET-altered Non Small Cell Lung Cancer.

Who makes pralsetinib?

Pralsetinib is being developed by Roche Holding AG, which trades under the ticker RHHBY. The drug is a small molecule kinase inhibitor in the -tinib class, and it is currently in Phase 1 clinical trials for RET-altered Non Small Cell Lung Cancer and other solid tumors.

What phase is pralsetinib in?

Pralsetinib is in Phase 1 clinical development. It is an investigational drug, meaning it has not been approved by regulatory authorities. The drug is being studied in a Phase 1/2 trial for RET-altered Non Small Cell Lung Cancer and other advanced solid tumors, with the trial now completed.

What clinical trials is pralsetinib in?

Pralsetinib is being studied in clinical trial NCT03037385, a Phase 1/2 study of the highly-selective RET inhibitor pralsetinib (BLU-667) in participants with thyroid cancer, non-small cell lung cancer, and other advanced solid tumors. The trial enrolled 590 participants and has been completed.

Is pralsetinib the same as BLU-667?

Yes, pralsetinib is also known as BLU-667. The clinical trial NCT03037385 refers to the drug as pralsetinib (BLU-667), confirming that both names refer to the same investigational RET inhibitor being developed by Roche for RET-altered cancers.