Combining Regorafenib and Pembrolizumab for MSI-H Colorectal Cancer

Randomized Trial of Regorafenib in Combination With Pembrolizumab or Pembrolizumab Monotherapy With an Efficacy Lead-in of Regorafenib and Pembrolizumab for Patients With MSI-H Colorectal Cancer

Phase 2 Interventional University of Pittsburgh · NCT06006923

This study is testing if combining two drugs, regorafenib and pembrolizumab, can help people with advanced MSI-H colorectal cancer have better treatment results.

Quick facts

PhasePhase 2
Study typeInterventional
Enrollment154 (estimated)
Ages18 Years and up
SexAll
SponsorUniversity of Pittsburgh Academic / other
Drugs / interventionspembrolizumab, chemotherapy, immunotherapy
Locations5 sites (Irvine, California and 4 other locations)
Trial IDNCT06006923 on ClinicalTrials.gov

What this trial studies

This trial investigates the combination of regorafenib, a multi-kinase inhibitor, with pembrolizumab, an anti-PD1 immune checkpoint inhibitor, for patients with advanced MSI-H colorectal cancer. The study consists of a lead-in phase to assess preliminary efficacy and safety, followed by a randomized phase to further evaluate the treatment's effectiveness. The rationale for this combination stems from preclinical and early clinical evidence suggesting that regorafenib may enhance the immune response when used alongside pembrolizumab. The goal is to improve treatment outcomes for patients who currently have limited options.

Who should consider this trial

Good fit: Ideal candidates include adults over 18 with histologically confirmed MSI-H colorectal cancer and measurable disease.

Not a fit: Patients with mismatch repair proficient (MSS) colorectal cancer are unlikely to benefit from this study.

Why it matters

Potential benefit: If successful, this combination could significantly enhance treatment efficacy for patients with MSI-H colorectal cancer.

How similar studies have performed: Previous studies have shown promising results with similar combinations of targeted therapies and immune checkpoint inhibitors in solid tumors.

Eligibility criteria

Show full inclusion / exclusion criteria
Inclusion Criteria:

1. Histologically confirmed mismatch repair deficient or microsatellite instability high advanced stage colorectal cancer
2. Measurable disease (per RECIST v1.1)
3. Eastern Cooperative Oncology Group (ECOG) performance status 0 to 1
4. Age \> 18
5. The patient must be able to swallow oral medication.
6. Adequate organ function based on the following lab assessments:

   1. ANC must be ≥ 1500/mm3
   2. platelet count must be ≥ 100,000/mm3
   3. WBC count ≥ 2.5 × 109 /L
   4. Hemoglobin must be ≥ 9 g/dL
   5. Alkaline phosphatase ≤ 2.5× upper limit of normal (ULN) with the exception of patients with documented liver or bone metastases who should have ALP ≤ 5.0× ULN
   6. AST and ALT ≤ 2.5× ULN with the exception of patients with documented liver metastases who may have AST and/or ALT ≤ 5.0× ULN
   7. International normalized ratio (INR) ≤ 1.5 x ULN and partial thromboplastin time (PTT) or activated partial thromboplastin time (aPTT) ≤ 1.5 x ULN unless receiving treatment with therapeutic anticoagulation
   8. Total bilirubin ≤ 1.5× ULN (≤ 3× ULN if Gilbert syndrome present)
   9. Serum albumin ≥ 2.8 g/dL or 28 g/L
   10. Creatinine clearance ≥ 50 mL/min (calculated using the Cockcroft-Gault formula) or creatinine ≤ 1.5× ULN
7. No more than three cycles of prior fluoropyrimidine-based chemotherapy including folinic acid, fluorouracil, and oxaliplatin (FOLFOX); folinic acid, fluorouracil, and irinotecan (FOLFIRI); and, folinic acid, fluorouracil, oxaliplatin, and irinotecan (FOLFOXIRI) excluding adjuvant treatment
8. Patients (male or female) of reproductive potential must agree to use an effective method of contraception (as discussed with treating physician) from the time consent is signed, during study therapy, and for at least 8 weeks after the last dose of study therapy.
9. Patients who received no more than 1 cycle of pembrolizumab monotherapy will be still eligible to be enrolled in lead in phase of the trial

Exclusion Criteria:

1. Prior anti-programmed death 1 (anti-PD-1) or anti-cytotoxic T-lymphocyte-associated antigen 4 (anti-CTLA-4) based therapy
2. More than 3 cycles of chemotherapy or progression of disease on first line therapy excluding adjuvant treatment and any systemic anticancer treatment within 2 weeks or 5 half-lives (whichever is shorter) prior to start of study treatment
3. Active autoimmune disease
4. Pregnant or lactating females
5. Uncontrolled human immunodeficiency virus (HIV), hepatitis B virus (HBV), and/or hepatitis C virus (HCV); patients with undetectable viral load and CD4 count \> 200 will be eligible for enrollment
6. Active untreated brain metastasis
7. Uncontrolled hypertension (HTN: systolic pressure \> 150 mmHg or diastolic pressure \> 90 mmHg on repeated measurements) and cardiovascular events within 12 months of start of treatment
8. Active infection or chronic infection requiring chronic suppressive antibiotics
9. No active cancer such as colon cancer other than adenocarcinoma (e.g., sarcoma, lymphoma, carcinoid) within 1 year
10. Patients with severe hepatic impairment (Child-Pugh C) are excluded as regorafenib has not been studied in this population and exposure might be increased in these patients
11. Major surgical procedure or significant traumatic injury within 28 days before start of study medication
12. Non-healing wound, non-healing ulcer, or non-healing bone fracture
13. Patients with evidence or history of any bleeding diathesis, irrespective of severity
14. Any hemorrhage or bleeding event ≥ CTCAE Grade 3 within 4 weeks prior to the start of study medication:

    1. Major surgical procedure or significant traumatic injury within 28 days before start of study medication
    2. Non-healing wound, non-healing ulcer, or non-healing bone fracture
    3. Patients with evidence or history of any bleeding diathesis, irrespective of severity
    4. Any hemorrhage or bleeding event ≥ CTCAE Grade 3 within 4 weeks prior to the start of study medication

Where this trial is running

Irvine, California and 4 other locations

Study contacts

How to participate

  1. Review the eligibility criteria above with your treating physician.
  2. Visit the official trial page on ClinicalTrials.gov for the most current contact information and recruitment status.
  3. Contact the listed study coordinator or principal investigator to request pre-screening. Pre-screening is free and never obligates you to enroll.
Conditions MSI-H Colorectal Cancermulti-kinase inhibitorreceptor tyrosine kinasesanti-PD1 blockadeimmune checkpoint inhibitorvascular endothelial growth factor receptor
Last reviewed 2026-06-13 by the Find a Trial editorial team. Information on this page is for educational purposes and is not medical advice. Always consult qualified healthcare professionals about clinical trial participation.