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Open-Label Safety and Tolerability Study of INCB057643 in Subjects With Advanced Malignancies

Registration Number
NCT02711137
Lead Sponsor
Incyte Corporation
Brief Summary

The purpose of the Study is to select a dose and assess the safety and tolerability of INCB057643 as a monotherapy (Part 1 and Part 2) and in combination with standard-of-care (SOC) agents (Part 3 and Part 4) for subjects with advanced malignancies.

Part 1 will determine the maximum tolerated dose of INCB057643 and/or a tolerated dose that demonstrates sufficient pharmacologic activity. Part 2 will further evaluate the safety, preliminary efficacy, PK, and PD of the dose(s) selected in Part 1 in select tumor types including solid tumors, lymphomas and other hematologic malignancies. Part 3 will determine the tolerated dose of INCB057643 in combination with select SOC agents; and assess the safety and tolerability of the combination therapy in select advanced solid tumors and hematologic malignancies. Part 4 will further evaluate the safety, preliminary efficacy, PK, and PD of the selected dose combination from Part 3 in 4 specific advanced solid tumor and hematologic malignancies.

Detailed Description

Not available

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
137
Inclusion Criteria
  • Histologically or cytologically confirmed diagnosis of relapsed or refractory advanced or metastatic malignancies:

    • Part 1: solid tumors or lymphomas, or hematologic malignancies
    • Part 2: histologically confirmed disease in specific tumor types
    • Part 3: advanced solid tumor or hematologic malignancy
    • Part 4: select advanced solid tumor or hematologic malignancy
  • For Part 1 and 2, subjects must have progressed following at least 1 line of prior therapy and there is no further established therapy that is known to provide clinical benefit (including subjects who are intolerant to the established therapy)

  • For Parts 3 and 4, subjects must have progressed following at least 1 line of prior therapy, and the treatment with the select SOC agent is relevant for the specific disease cohort.

  • Life expectancy > 12 weeks, for MF subjects in Parts 3 and 4, life expectancy > 24 weeks

  • Eastern Cooperative Oncology Group (ECOG) performance status

    • Parts 1 and 3: 0 or 1
    • Parts 2 and 4: 0, 1, or 2
  • Willingness to avoid pregnancy or fathering children

Exclusion Criteria
  • Inadequate bone marrow function per protocol-specified hemoglobin, platelet count, and absolute neutrophil count
  • Inadequate organ function per protocol-specified total bilirubin, AST and ALT, creatinine clearance and alkaline phosphatase.
  • Receipt of anticancer medications or investigational drugs within protocol-specified intervals
  • Unless approved by the medical monitor, may not have received an allogeneic hematopoietic stem cell transplant within 6 months before treatment, or have active graft-versus-host-disease following allogeneic transplant
  • Unless approved by the medical monitor, may not have received autologous hematopoietic stem cell transplant within 3 months before treatment
  • Any unresolved toxicity ≥ Grade 2 (except stable Grade 2 peripheral neuropathy or alopecia) from previous anticancer therapy
  • Radiotherapy within the 2 weeks before initiation of treatment. Palliative radiation treatment to nonindex or bone lesions performed less than 2 weeks before treatment initiation may be considered with medical monitor approval
  • Currently active and uncontrolled infectious disease requiring systemic antibiotic, antifungal, or antiviral treatment
  • Untreated brain or central nervous system (CNS) metastases or brain/CNS metastases that have progressed
  • History or presence of abnormal electrocardiogram (ECG) that, in the investigator's opinion, is clinically meaningful
  • Type 1 diabetes or uncontrolled Type 2 diabetes
  • HbA1c of ≥ 8% (all subjects will have HbA1c test at screening)
  • Any sign of clinically significant bleeding
  • Coagulation panel within protocol-specified parameters

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
Part1/Treatment Group A : 16mg QD INCB057643INCB057643Initial cohort dose of INCB057643 monotherapy at the protocol specified starting dose in the TGA. Treatment Group A included solid tumors and lymphoma
Part1/Treatment Group A : 8mg QD INCB057643INCB057643Initial cohort dose of INCB057643 monotherapy at the protocol specified starting dose in the TGA. Treatment Group A included solid tumors and lymphoma
Part1/Treatment Group A : 12mg QD INCB057643INCB057643Initial cohort dose of INCB057643 monotherapy at the protocol specified starting dose in the TGA. Treatment Group A included solid tumors and lymphoma
Part1/Treatment Group B : 8mg QD INCB057643INCB057643Initial cohort dose of INCB054763 monotherapy at the protocol-specified cohort escalation treatment group B (TGB), based on protocol-specific criteria. Treatment Group B included any acute leukemia, HRMDS, MDS/MPN, or MF
Part1/Treatment Group B : 12mg QD INCB057643INCB057643Initial cohort dose of INCB054763 monotherapy at the protocol-specified cohort escalation treatment group B (TGB), based on protocol-specific criteria. Treatment Group B included any acute leukemia, HRMDS, MDS/MPN, or MF.
Part1/Treatment Group C : 8mg QD INCB057643INCB057643Initial cohort dose of INCB054763 monotherapy at the protocol-specified cohort escalation treatment group C (TGC), based on protocol-specific criteria. Treatment Group C includes subjects with MM
Part2/Treatment Group A : 12 mg INCB057643 Expansion CohortINCB057643Initial cohort dose of INCB054763 monotherapy at the specified RP2D dose selected in Part 1 cohort escalation treatment group A (TGA), based on protocol-specific criteria. Part 2 Treatment Group A expansion included pancreatic adenocarcinoma, castration-resistant prostrate cancer, breast cancer, high grade serious ovarian cancer, glioblastoma multiform, non-hodgkin's lymphoma, ewing's sarcoma, and solid tumor or lymphoma.
Part2/Treatment Group B : 12 mg INCB057643 Expansion CohortINCB057643Initial cohort dose of INCB057463 monotherapy at the specified RP2D dose selected in Part 1 cohort escalation treatment group B (TGB), based on protocol-specific criteria. Part 2 Treatment Group B expansion included pancreatic adenocarcinoma, castration-resistant prostrate cancer, breast cancer, high grade serious ovarian cancer, glioblastoma multiform, non-hodgkin's lymphoma, ewing's sarcoma, and solid tumor or lymphoma.
Part3/Treatment Group A : 8 mg INCB057643 + Gemcitabine 1000mgINCB057643Initial cohort dose of INCB057643 monotherapy based on protocol-specific criteria. Part 3 will determine the MTD and/or a tolerated dose of the combination of INCB057643 and one of the SOC agents (Gemcitabine) in relapsed or refractory advanced or metastatic solid tumors and hematologic malignancies where Gemcitabine is relevant
Part3/Treatment Group B : 8 mg INCB057643 + Paclitaxel 80mgINCB057643Initial cohort dose of INCB054763 monotherapy based on protocol-specific criteria. Part 3 will determine the MTD and/or a tolerated dose of the combination of INCB057643 and one of the SOC agents (Paclitaxel) in relapsed or refractory advanced or metastatic solid tumors and hematologic malignancies.
Part3/Treatment Group C : 8 mg INCB057643 + Rucaparib 600mgINCB057643Initial cohort dose of INCB054763 monotherapy based on protocol-specific criteria. Part 3 will determine the MTD and/or a tolerated dose of the combination of INCB057643 and one of the SOC agents (Rucaparib) in relapsed or refractory advanced or metastatic solid tumors and hematologic malignancies.
Part3/Treatment Group D : 8 mg INCB057643 + Abir +PredniINCB057643Initial cohort dose of INCB054763 monotherapy based on protocol-specific criteria. Part 3 will determine the MTD and/or a tolerated dose of the combination of INCB057643 and one of the SOC agents (Abiraterone + Prednisone) in Castration Resistant Prostrate Cancer
Part3/Treatment Group E : 8 mg INCB057643 + Ruxolitinib 20mgINCB057643Initial cohort dose of INCB054763 monotherapy based on protocol-specific criteria. Part 3 will determine the MTD and/or a tolerated dose of the combination of INCB057643 and one of the SOC agents (Ruxolitinib) in Myelofibrosis.
Part3/Treatment Group F : 8 mg INCB057643 + Azacitidine 75mgINCB057643Initial cohort dose of INCB054763 monotherapy based on protocol-specific criteria. Part 3 will determine the MTD and/or a tolerated dose of the combination of INCB057643 and one of the SOC agents (Azacitidine) in Acute Myeloid Leukemia and Myelodysplastic Syndrome
Part3/Treatment Group A : 8 mg INCB057643 + Gemcitabine 1000mgGemcitabineInitial cohort dose of INCB057643 monotherapy based on protocol-specific criteria. Part 3 will determine the MTD and/or a tolerated dose of the combination of INCB057643 and one of the SOC agents (Gemcitabine) in relapsed or refractory advanced or metastatic solid tumors and hematologic malignancies where Gemcitabine is relevant
Part3/Treatment Group C : 8 mg INCB057643 + Rucaparib 600mgRucaparibInitial cohort dose of INCB054763 monotherapy based on protocol-specific criteria. Part 3 will determine the MTD and/or a tolerated dose of the combination of INCB057643 and one of the SOC agents (Rucaparib) in relapsed or refractory advanced or metastatic solid tumors and hematologic malignancies.
Part3/Treatment Group B : 8 mg INCB057643 + Paclitaxel 80mgPaclitaxelInitial cohort dose of INCB054763 monotherapy based on protocol-specific criteria. Part 3 will determine the MTD and/or a tolerated dose of the combination of INCB057643 and one of the SOC agents (Paclitaxel) in relapsed or refractory advanced or metastatic solid tumors and hematologic malignancies.
Part3/Treatment Group D : 8 mg INCB057643 + Abir +PredniAbirateroneInitial cohort dose of INCB054763 monotherapy based on protocol-specific criteria. Part 3 will determine the MTD and/or a tolerated dose of the combination of INCB057643 and one of the SOC agents (Abiraterone + Prednisone) in Castration Resistant Prostrate Cancer
Part3/Treatment Group E : 8 mg INCB057643 + Ruxolitinib 20mgRuxolitinibInitial cohort dose of INCB054763 monotherapy based on protocol-specific criteria. Part 3 will determine the MTD and/or a tolerated dose of the combination of INCB057643 and one of the SOC agents (Ruxolitinib) in Myelofibrosis.
Part3/Treatment Group F : 8 mg INCB057643 + Azacitidine 75mgAzacitidineInitial cohort dose of INCB054763 monotherapy based on protocol-specific criteria. Part 3 will determine the MTD and/or a tolerated dose of the combination of INCB057643 and one of the SOC agents (Azacitidine) in Acute Myeloid Leukemia and Myelodysplastic Syndrome
Primary Outcome Measures
NameTimeMethod
Number of Participants With Treatment Emergent Adverse Events (TEAE's).From screening through at least 30 days after end of treatment, up to approximately 24 months

Adverse events reported for the first time or worsening of a pre-existing event after first dose of study drug/treatment.

Secondary Outcome Measures
NameTimeMethod
AUC0-t: Area Under the Single-dose Plasma Concentration-time Curve of INCB057643Predose, 0.5, 1, 2, 4, 6, 8 hours on C1D1

Area under the single-dose plasma concentration-time curve from Hour 0 to the last quantifiable measurable plasma concentration of INCB057643 administered as monotherapy in fasted state

AUC0-24: Area Under the Steady-state Plasma Concentration-time Curve of INCB057643 Administered as MonotherapyC2D1

Area under the steady-state plasma concentration-time curve over 1 dosing interval from Hour 0 to 24 for QD administration of INCB057643 administered as monotherapy in fed state.

Part 2 - Cmax: Maximum Observed Plasma Concentration of INCB057643.C2D1

Maximum Observed Plasma Concentration INCB057643 administered as monotherapy in fed state.

Objective Response Rate (ORR) With INCB057643 in Solid TumorsEfficacy measures from screening through end of treatment and follow-up (every 9 weeks), up to approximately 24 months

Objective response rate is defined as the proportion of subjects who have an objective response using the applicable disease assessment criteria. ORR was proportion of participants with best overall response \[complete response (CR) or partial response (PR)\].

Tmax: Time to Maximum Plasma Concentration of INCB057643Predose, 0.5, 1, 2, 4, 6, 8 hours on C1D1 and C1D8

Time to maximum plasma concentration of INCB057643 administered as monotherapy in fasted state

Percent Inhibition of Total Cellular Myc Protein Concentrations Before and After Administration of INCB057643 When Administered as Monotherapy in an Ex-vivo AssayPD in plasma at pre-dose and 0.5, 1, 2, 4, 6 and 8 hours postdose, for C1D1 and C1D8, and 24hrs post dose for C1D1

An ex vivo assay (utilized in monotherapy only), Measuring Total c-Myc protein expressed from an exogenously added cell line (KMS12BM) to patient plasma, before and after administration of INCB057643.

Part 2-Tmax: Time to Maximum Plasma Concentration of INCB057643C2D1

Time to maximum plasma concentration of INCB057643 administered as monotherapy in fed state

Cmax: Maximum Observed Plasma Concentration of INCB057643.Predose, 0.5, 1, 2, 4, 6, 8 hours on C1D1 and C1D8

Maximum Observed Plasma Concentration INCB057643 administered as monotherapy in fasted state.

Trial Locations

Locations (18)

Yale University

🇺🇸

New Haven, Connecticut, United States

Hematology - Oncology Associates of Treasure Coast

🇺🇸

Port Saint Lucie, Florida, United States

The Methodist Hospital

🇺🇸

Houston, Texas, United States

Wake Forest Baptist Health

🇺🇸

Winston-Salem, North Carolina, United States

MultiCare Institute for Research and Innovation

🇺🇸

Tacoma, Washington, United States

University of California

🇺🇸

La Jolla, California, United States

University of Alabama

🇺🇸

Birmingham, Alabama, United States

University of Rochester, Wilmot Cancer Center

🇺🇸

Rochester, New York, United States

University of North Carolina at Chapel Hill

🇺🇸

Chapel Hill, North Carolina, United States

Washington University

🇺🇸

Saint Louis, Missouri, United States

Oncology Consultants, P.A.

🇺🇸

Houston, Texas, United States

HÔPITAL SAINT-LOUIS, Service Hématologie Adultes

🇫🇷

Paris, France

Sarah Cannon Research Institute at Health One

🇺🇸

Denver, Colorado, United States

Huntsman Cancer Institute

🇺🇸

Salt Lake City, Utah, United States

Sylvester Comprehensive Cancer Center

🇺🇸

Miami, Florida, United States

Institut Jules Bordet, Clinical Trial Conduct Unit

🇧🇪

Brussels, Belgium

University of Michigan

🇺🇸

Ann Arbor, Michigan, United States

University of Minnesota

🇺🇸

Minneapolis, Minnesota, United States

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