What side effects are associated with this type of intervention?

Common treatments for Gastrointestinal Stromal Tumor (GIST) using tyrosine kinase inhibitors (TKIs) like imatinib, sunitinib, and regorafenib often result in side effects such as fatigue, diarrhea, nausea, hypertension, hand-foot syndrome, and liver toxicity. Severe but less common side effects can include cardiac toxicity, gastrointestinal perforations, and severe skin reactions. These side effects are important to consider for effective management of the treatment plan.

What prior FDA approvals exist?

Several tyrosine kinase inhibitors (TKIs) have been approved by the FDA for the treatment of Gastrointestinal Stromal Tumor (GIST). Imatinib was the first TKI approved, targeting KIT and PDGFRA mutations. Sunitinib and regorafenib were subsequently approved for patients with imatinib-resistant GIST. Avapritinib and ripretinib are newer TKIs specifically targeting PDGFRA D842V mutations and other resistant forms of GIST. These drugs focus on inhibiting specific pathways involved in GIST, similar to the investigational drug THE-630.

What other types of research exist?

Promising novel alternatives to THE-630 for GIST patients include regorafenib, cabozantinib, sorafenib, and lenvatinib. These multitargeted kinase inhibitors have shown some efficacy in advanced GIST. Additionally, investigational agents such as larotrectinib and entrectinib, which target specific genetic alterations like NTRK fusions, may also be considered based on the tumor's molecular profile.

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Kinase Inhibitor

THE-630 for Gastrointestinal Stromal Tumors

Phase 1 & 2

Waitlist Available

Research Sponsored by Theseus Pharmaceuticals

Eligibility Criteria Checklist

Specific guidelines that determine who can or cannot participate in a clinical trial

Must have

Be older than 18 years old

Timeline

Screening 3 weeks

Treatment Varies

Follow Up cycle 1 day 1 and cycle 1 day 15 (each cycle is 28 days)

Awards & highlights

No Placebo-Only Group

Summary

This trial is testing THE-630, a pill that blocks a protein helping cancer cells grow, in patients with advanced GIST who haven't responded to other treatments. The goal is to see if it is safe and effective.

Who is the study for?

This trial is for adults with advanced gastrointestinal stromal tumors (GIST) who have not responded to or cannot tolerate certain treatments like imatinib, sunitinib, regorafenib, and others. Participants must be in good health otherwise, with no serious heart conditions or uncontrolled infections. Women of childbearing age and men with partners of childbearing potential must agree to use effective contraception.

What is being tested?

The study is testing the safety and effectiveness of a drug called THE-630 on patients with GIST. It will also look at how the body processes the drug. The trial includes different phases where doses may vary based on patient response and side effects.

What are the potential side effects?

While specific side effects for THE-630 are not listed here, common side effects from cancer drugs can include nausea, fatigue, diarrhea, risk of infection due to low blood cell counts, liver problems, skin reactions among others.

Timeline

Screening ~ 3 weeks3 visits

Treatment ~ Varies

Follow Up ~ cycle 1 day 1 and cycle 1 day 15 (each cycle is 28 days)

Screening ~ 3 weeks

Treatment ~ Varies

Follow Up ~cycle 1 day 1 and cycle 1 day 15 (each cycle is 28 days)

This trial's timeline: 3 weeks for screening, Varies for treatment, and cycle 1 day 1 and cycle 1 day 15 (each cycle is 28 days) for reporting.

Treatment Details

Study Objectives

Study objectives can provide a clearer picture of what you can expect from a treatment.

Primary study objectives

Dose Escalation (Phase 1): Recommended Phase 2 Dose (RP2D) of Orally Administered THE-630

Dose Escalation (Phase 1): Safety Analysis - Maximum Tolerated Dose (MTD) of Orally Administered THE-630

Secondary study objectives

Dose Escalation (Phase 1): Plasma PK Parameters of THE-630 and Its Active Metabolite - AUC 0-24 (Area Under the Concentration-time Curve From Time Zero to 24 Hours)

Dose Escalation (Phase 1): Plasma PK Parameters of THE-630 and Its Active Metabolite - AUC 0-t (Area Under the Concentration-time Curve From Time Zero to Time t)

Dose Escalation (Phase 1): Plasma PK Parameters of THE-630 and Its Active Metabolite - Tmax (Time of First Occurrence of Cmax)

+5 more

Awards & Highlights

No Placebo-Only Group

All patients enrolled in this study will receive some form of active treatment.

Trial Design

4Treatment groups

Experimental Treatment

Group I: Expansion Cohort 3Experimental Treatment1 Intervention

Patients with unresectable or metastatic GIST who have progressed on or are intolerant to imatinib (including in the adjuvant setting) and who have not received additional systemic therapy for advanced GIST, who will receive orally administered THE-630 at the recommended Phase 2 dose based on the dose escalation phase.

Group II: Expansion Cohort 2Experimental Treatment1 Intervention

Patients with unresectable or metastatic GIST who have progressed on or are intolerant to imatinib, sunitinib and 0-1 additional lines of therapy in the advanced/metastatic setting, who will receive orally administered THE-630 at the recommended Phase 2 dose based on the dose escalation phase.

Group III: Expansion Cohort 1Experimental Treatment1 Intervention

Patients with unresectable or metastatic GIST who have progressed on or are intolerant to imatinib, sunitinib, regorafenib and ripretinib who will receive orally administered THE-630 at the recommended Phase 2 dose based on the dose escalation phase.

Group IV: Dose EscalationExperimental Treatment1 Intervention

Participants with unresectable or metastatic GIST who will receive orally administered THE-630.

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Research Highlights

Information in this section is not a recommendation. We encourage patients to speak with their healthcare team when evaluating any treatment decision.

Mechanism Of Action

Side Effect Profile

Prior Approvals

Other Research

The most common treatments for Gastrointestinal Stromal Tumor (GIST) involve tyrosine kinase inhibitors (TKIs) such as imatinib, sunitinib, and regorafenib. These drugs target specific mutations in the KIT and PDGFRA genes, which are responsible for the abnormal activation of signaling pathways that drive tumor growth. By inhibiting these kinases, TKIs effectively reduce tumor proliferation and induce apoptosis. This is particularly important for GIST patients as these targeted therapies offer a more effective treatment option compared to conventional chemotherapy, especially for those with advanced or metastatic disease. Additionally, understanding the specific mutations in a patient's tumor can help tailor the treatment plan and manage resistance to therapy, improving overall outcomes.