A Phase 1/2 Study of CPI-0610 With and Without Ruxolitinib in Patients With Hematologic and Myeloproliferative Malignancies

NCT ID: NCT02158858

Last Updated: 2025-10-08

Study Results

Results pending

The study team has not published outcome measurements, participant flow, or safety data for this trial yet. Check back later for updates.

Basic Information

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Recruitment Status

COMPLETED

Clinical Phase

PHASE1/PHASE2

Total Enrollment

336 participants

Study Classification

INTERVENTIONAL

Study Start Date

2014-07-16

Study Completion Date

2025-01-09

Brief Summary

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Phase 1 Part: Open-label, sequential dose escalation study of pelabresib (CPI-0610) in patients with previously treated Acute Leukemia, Myelodysplastic/Myeloproliferative Neoplasms, and Phase 2 Part: Open-label study of pelabresib (CPI-0610) with and without Ruxolitinib in patients with Myeloproliferative Neoplasms (Myelofibrosis and Essential Thrombocythemia).

Pelabresib (CPI-0610) is a small molecule inhibitor of bromodomain and extra-terminal (BET) proteins.

Detailed Description

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Conditions

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Myelofibrosis Leukemia, Myelocytic, Acute Myelodysplastic/Myeloproliferative Neoplasm Myelodysplastic Syndrome (MDS) Preleukemia Primary Myelofibrosis Myeloproliferative Disorders Bone Marrow Disease Hematological Disease Precancerous Conditions Neoplasms Leukemia Neoplasms by Histologic Type Essential Thrombocytosis

Study Design

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Allocation Method

NON_RANDOMIZED

Intervention Model

PARALLEL

Primary Study Purpose

TREATMENT

Blinding Strategy

NONE

Study Groups

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Phase 1

Patients are enrolled in sequential cohorts (acute leukemia, including acute myelogenous leukemia (AML), acute lymphocytic leukemia (ALL), and acute undifferentiated or biphenotypic leukemia; chronic myelogenous leukemia (CML) in blast crisis; myelodysplastic syndrome (MDS); myelodysplastic/myeloproliferative neoplasms (MDS/MPN); or myelofibrosis (MF)) and receive escalating doses of pelabresib (CPI-0610).

Group Type EXPERIMENTAL

Pelabresib

Intervention Type DRUG

CPI-0610 is administered orally once daily for 14 consecutive days, followed by a 7-day break (1 cycle = 21 days)

Phase 2 (Arm 1): Prior JAKi Monotherapy Arm (MF patients treated with pelabresib alone)

* Cohort 1A: Open to patients with MF who are Transfusion Dependent (TD) and who have previously been treated with a JAKi and are intolerant, resistant, refractory or lost response to the JAKi, or are ineligible to be treated with a JAKi (pelabresib (CPI-0610) alone)
* Cohort 1B: Open to patients with MF who are not TD and who have previously been treated with a JAKi and are intolerant, resistant, refractory or lost response to the JAKi, or are ineligible to be treated with a JAKi. (pelabresib (CPI-0610) alone)

Group Type EXPERIMENTAL

Pelabresib

Intervention Type DRUG

CPI-0610 is administered orally once daily for 14 consecutive days, followed by a 7-day break (1 cycle = 21 days)

Phase 2 (Arm 2): Prior JAKi Combination Arm

* Cohort 2A: Open to patients with MF who are Transfusion Dependent (TD) and are currently taking ruxolitinib but have disease that is not being adequately controlled by ruxolitinib (pelabresib (CPI-0610) + Ruxolitinib)
* Cohort 2B: Open to patients with MF who are not TD and are currently taking ruxolitinib but have disease that is not being adequately controlled by ruxolitinib. (pelabresib (CPI-0610) + Ruxolitinib)

Group Type EXPERIMENTAL

Pelabresib

Intervention Type DRUG

CPI-0610 is administered orally once daily for 14 consecutive days, followed by a 7-day break (1 cycle = 21 days)

Ruxolitinib

Intervention Type DRUG

Ruxolitinib is given orally, twice daily (BID), on a continuous basis for 21 consecutive days of each 21-day cycle.

Phase 2 (Arm 3): JAKi Naïve Combination Arm

Open to patients with MF who have not previously received a JAKi (pelabresib (CPI-0610) + Ruxolitinib)

Group Type EXPERIMENTAL

Pelabresib

Intervention Type DRUG

CPI-0610 is administered orally once daily for 14 consecutive days, followed by a 7-day break (1 cycle = 21 days)

Ruxolitinib

Intervention Type DRUG

Ruxolitinib is given orally, twice daily (BID), on a continuous basis for 21 consecutive days of each 21-day cycle.

Phase 2 (Arm 4): Essential Thrombocythemia (ET) Monotherapy Arm

Open to high-risk patients with ET who are resistant or intolerant to hydroxyurea (HU) (pelabresib (CPI-0610) alone)

Group Type EXPERIMENTAL

Pelabresib

Intervention Type DRUG

CPI-0610 is administered orally once daily for 14 consecutive days, followed by a 7-day break (1 cycle = 21 days)

Interventions

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Pelabresib

CPI-0610 is administered orally once daily for 14 consecutive days, followed by a 7-day break (1 cycle = 21 days)

Intervention Type DRUG

Ruxolitinib

Ruxolitinib is given orally, twice daily (BID), on a continuous basis for 21 consecutive days of each 21-day cycle.

Intervention Type DRUG

Other Intervention Names

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CPI-0610 DAK539

Eligibility Criteria

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Inclusion Criteria

* Age: Adults ≥18 years.
* Diagnosis: Histologically or cytologically confirmed diagnosis of one of the following hematologic malignancies:

* Acute myelogenous leukemia (AML)
* Acute lymphocytic leukemia (ALL)
* Acute undifferentiated or biphenotypic leukemia
* Chronic myeloid leukemia (CML) in blast crisis
* Myelodysplastic syndrome (MDS)
* Myelodysplastic/myeloproliferative neoplasms (MDS/MPN)
* Myelofibrosis (MF)
* Performance Status: ECOG ≤2.
* Organ Function:

* Serum total bilirubin ≤1.5 × ULN
* AST/ALT ≤2.5 × ULN (up to 5 × ULN if due to leukemic infiltration)
* Serum creatinine ≤2.0 × ULN or CrCl ≥30 mL/min
* Hematology (MF only):

* Platelet count ≥50 × 10⁹/L and ANC ≥1 × 10⁹/L (MF not on ruxolitinib)
* Platelet count ≥75 × 10⁹/L and ANC ≥1 × 10⁹/L (MF on ruxolitinib)
* Other:

* DIPSS-plus risk category of intermediate-2 or high (MF only)
* Serum glucose ≤160 mg/dL (or HbA1C ≤7%)
* Fully recovered from major surgery and acute toxic effects of prior therapy
* Negative pregnancy test for women of childbearing potential
* Agreement to use appropriate contraception
* Written informed consent

1. MF Arms (Prior JAKi, Add-on JAKi, JAKi Naïve)

* Age: Adults ≥18 years
* Diagnosis: Confirmed primary MF or MF evolved from ET or PV
* Risk: DIPSS intermediate-2 or higher
* Platelets:

* ≥75 × 10⁹/L (Arms 1 \& 2)
* ≥100 × 10⁹/L (Arm 3, JAKi naïve)
* ANC: ≥1 × 10⁹/L
* Spleen Volume: ≥450 cm³ by MRI/CT (non-TD cohorts) OR
* Transfusion Dependence: Average ≥2 RBC transfusions/month (total ≥6 in prior 12 weeks) for TD cohorts
* Peripheral Blood Blasts: \<10%
* Symptoms: At least 2 symptoms measurable (score ≥1 for Arms 1 \& 2; score ≥3 or total ≥10 for Arm 3) using MFSAF v4.0
* Treatment History:

* Arm 1 (Prior JAKi): Previously treated with JAKi and intolerant, resistant, refractory, or lost response, or ineligible for JAKi
* Arm 2 (Add-on JAKi): On ruxolitinib ≥6 months, stable dose ≥8 weeks, not adequately controlled
* Arm 3 (JAKi Naïve): No prior JAKi, eligible for ruxolitinib
* Performance Status: ECOG ≤2
* Organ Function: Serum direct bilirubin \<2 × ULN, AST/ALT ≤2.5 × ULN (up to 5 × ULN if due to liver involvement), CrCl ≥45 mL/min
* Other: Fully recovered from major surgery/acute toxic effects, effective contraception, written informed consent
2. ET Arm (High-Risk ET)

* Age: Adults ≥18 years
* Diagnosis: Confirmed ET (WHO 2016 criteria)
* High-Risk: At least one of:

* Age \>60 years
* Platelets \>1500 × 10⁹/L
* Prior thrombosis, erythromelalgia, or migraine (disease-related)
* Prior hemorrhage related to ET
* Diabetes/hypertension requiring therapy \>6 months
* Symptoms: ≥2 symptoms with average score ≥3 or total score ≥15 (MPN-SAF)
* Platelets: \>600 × 10⁹/L
* Resistant/Intolerant to HU: As defined by ELN
* Performance Status: ECOG ≤2
* Life Expectancy: \>24 weeks
* ANC: ≥1 × 10⁹/L
* Organ Function: Serum direct bilirubin \<2 × ULN, AST/ALT ≤2.5 × ULN, CrCl ≥45 mL/min
* Other: Fully recovered from major surgery/acute toxic effects, effective contraception, written informed consent

Exclusion Criteria

* Untreated newly diagnosed acute leukemia (unless AML with myelodysplasia-related changes and 20-30% blasts)
* Relapsed/refractory acute leukemia where further induction chemotherapy is beneficial
* Acute leukemia relapse \<6 months after allogeneic SCT
* CML in blast crisis treated with only one TKI
* Very low/low risk MDS without prior treatment
* CNS involvement by leukemia (unless resolved)
* Active HIV, Hepatitis B or C infection
* GI impairment affecting absorption (unresolved nausea, vomiting, diarrhea \>CTCAE grade 1)
* Significant cardiac disease (recent MI/angina, high cTn, QTcF \>470 ms, LVEF \<50%, uncontrolled arrhythmia, etc.)
* Severe/uncontrolled comorbidities
* Recent systemic anti-cancer therapy (other than hydroxyurea/radiotherapy) \<2 weeks prior
* Ongoing or recent JAK inhibitor use (\<2 weeks prior, MF only)
* Recent therapeutic antibody (\<4 weeks) or investigational agent (\<2 weeks or \<5 half-lives)
* Use of strong CYP450 inhibitors/inducers or drugs with Torsades de Pointes risk
* Immunosuppressive treatment that cannot be discontinued
* Pregnant/lactating women
* Inadequate contraception
* Inability/unwillingness to comply with protocol



* Prior splenectomy (MF non-TD cohorts)
* Splenic irradiation within 3 months
* Active or chronic HIV, Hepatitis B/C infection
* Active clinically significant infection (until recovery ≥2 weeks)
* Anemia deemed clinically significant (iron/B12/folate deficiency, hemolytic anemia)
* Major bleeding event (≥2 g/dL Hgb drop or ≥2 units transfused in last 6 months)
* Liver cirrhosis Child-Pugh B or C
* GI impairment affecting absorption (unresolved nausea, vomiting, diarrhea \>CTCAE grade 1)
* Rare hereditary problems of galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption (Arm 3)
* Hypersensitivity to ruxolitinib formulation (Arm 3)
* History of PML (Arm 3)
* Significant cardiac disease (recent MI/angina, QTcF \>500 ms \[\>450 ms in France/Germany\], uncontrolled arrhythmia, etc.)
* Ongoing uncontrolled hypertension
* Severe/uncontrolled comorbidities
* Systemic anticancer treatment (other than ruxolitinib for Arm 2, HU/ANA up to 24h prior) \<2 weeks or \<5 half-lives prior
* Prior treatment with any BET inhibitor
* Hematopoietic growth factor or androgenic steroids \<4 weeks prior
* Systemic corticosteroids ≥10 mg prednisone equivalent within 4 weeks (exceptions for short courses)
* Concurrent/second malignancy (except certain adequately treated cancers)
* Pregnant/lactating women, or planning pregnancy within protocol-defined window
* Inability/unwillingness to comply with protocol
Minimum Eligible Age

18 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

No

Sponsors

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The Leukemia and Lymphoma Society

OTHER

Sponsor Role collaborator

Constellation Pharmaceuticals

INDUSTRY

Sponsor Role lead

Responsible Party

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Responsibility Role SPONSOR

Principal Investigators

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Novartis Pharmaceuticals

Role: STUDY_DIRECTOR

Novartis Pharmaceuticals

Locations

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Mayo Clinic Arizona

Phoenix, Arizona, United States

Site Status

UCLA Medical Center

Los Angeles, California, United States

Site Status

Mayo Clinic Jacksonville

Jacksonville, Florida, United States

Site Status

Northwestern University - Lurie Comprehensive Cancer Center

Chicago, Illinois, United States

Site Status

Massachusetts General Hospital Cancer Center

Boston, Massachusetts, United States

Site Status

University of Michigan Medical Center

Ann Arbor, Michigan, United States

Site Status

Washington University School of Medicne Neuromuscular Division Department of Neurology Research

St Louis, Missouri, United States

Site Status

Memorial Sloan Kettering Cancer Center

New York, New York, United States

Site Status

ICAHN School of Medicine at Mount Sinai

New York, New York, United States

Site Status

Weill Medical College and New York Presbyterian Hospital

New York, New York, United States

Site Status

The University of Texas MD Anderson Cancer Center

Houston, Texas, United States

Site Status

Froedtert & Medical College of Wisconsin

Milwaukee, Wisconsin, United States

Site Status

UZ Leuven - Campus Gasthuisberg

Leuven, Viaams Braban, Belgium

Site Status

AZ Sint-Jan Burgge-Oostende AV- Campus Sint-Jan

Bruges, West-Vlaanderen, Belgium

Site Status

ZNA Stuyvenberg Antwerpen

Antwerp, , Belgium

Site Status

University of Alberta Hospital

Edmonton, Alberta, Canada

Site Status

St. Paul's Hospital

Vancouver, British Columbia, Canada

Site Status

Juravinski Cancer Centre

Hamilton, Ontario, Canada

Site Status

Princess Margaret Cancer Centre

Toronto, Ontario, Canada

Site Status

Jewish General Hospital

Montreal, Quebec, Canada

Site Status

Institut de cancérologie du Gard - Hematologie clinique

Nîmes, Gard, France

Site Status

CHRU de Lille - Hopital Claude Huriez

Toulouse, Haute-Garonne, France

Site Status

CHRU de Lille - Hopital Claude Huriez - Maladies du Sang

Lille, Hauts-de-France, France

Site Status

CHU - Hopital Saint Louis - Centre D'Investigations Clinique

Paris, , France

Site Status

Institut Gustave Roussy

Villejuif, Île-de-France Region, France

Site Status

Universitätsklinikum Bonn

Bonn, North Rhine-Westphalia, Germany

Site Status

Universitätsklinikum Leipzig AöR

Leipzig, Saxony, Germany

Site Status

Institue of Hematology "L. and A. Seràgnoli"

Bologna, Emilia-Romagna, Italy

Site Status

Servizio Sanitario Regionale Emilia-Romagna - Azienda Unita Sanitaria Locale (AUSL) di Rimini - Ospedale Infermi di Rimini

Rimini, Emilia-Romagna, Italy

Site Status

AOU S.Martino, IRCCS, IST-Istituto Nazionale Ricerca Sul Can

Genoa, Liguria, Italy

Site Status

Ospedale Maggiore Policlinico, Fondazione IRCCS Ca' Granda

Milan, Lombardy, Italy

Site Status

IRCCS Policlinico San Matteo, Università degli studi di Pavi

Pavia, Lombardy, Italy

Site Status

Ospedale di Circolo, PO Varese, AO Ospedale di Circolo e Fon

Varese, Lombardy, Italy

Site Status

Azienda Ospedaliero-Universitaria Careggi

Florence, , Italy

Site Status

AOU Maggiore della Carità

Novara, , Italy

Site Status

Maastricht University Medical Center

Maastricht, Limburg, Netherlands

Site Status

VUmcResearch B.V.

Amsterdam, North Holland, Netherlands

Site Status

Erasmus Universitair Medisch Centrum Rotterdam

Rotterdam, South Holland, Netherlands

Site Status

Instytut Hematologii i Transfuzjologii w Warszawie

Warsaw, Masovian Voivodeship, Poland

Site Status

Uniwersyteckie Centrum Kliniczne

Gdansk, Pomeranian Voivodeship, Poland

Site Status

Oxford University Hospitals

Headington, Oxford, United Kingdom

Site Status

Belfast City Hospital

Belfast, , United Kingdom

Site Status

University of Cambridge

Cambridge, , United Kingdom

Site Status

University Hospital of Wales

Cardiff, , United Kingdom

Site Status

Beatson West of Scotland Cancer Centre

Glasgow, , United Kingdom

Site Status

University College London Hospital's NHS foundation Trust

London, , United Kingdom

Site Status

Guys and St Thomas' Hospital - Haematology

London, , United Kingdom

Site Status

The Christie Hospital

Manchester, , United Kingdom

Site Status

Countries

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United States Belgium Canada France Germany Italy Netherlands Poland United Kingdom

References

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Stein EM, Fathi AT, Harb WA, Colak G, Fusco A, Mangan JK. Results from phase 1 of the MANIFEST clinical trial to evaluate the safety and tolerability of pelabresib in patients with myeloid malignancies. Leuk Lymphoma. 2024 Apr;65(4):503-510. doi: 10.1080/10428194.2023.2300710. Epub 2024 Jan 23.

Reference Type DERIVED
PMID: 38259250 (View on PubMed)

Gupta V, Mascarenhas J, Kremyanskaya M, Rampal RK, Talpaz M, Kiladjian JJ, Vannucchi AM, Verstovsek S, Colak G, Dey D, Harrison C. Matching-adjusted indirect comparison of the pelabresib-ruxolitinib combination vs JAKi monotherapy in myelofibrosis. Blood Adv. 2023 Sep 26;7(18):5421-5432. doi: 10.1182/bloodadvances.2023010628.

Reference Type DERIVED
PMID: 37530627 (View on PubMed)

Mascarenhas J, Kremyanskaya M, Patriarca A, Palandri F, Devos T, Passamonti F, Rampal RK, Mead AJ, Hobbs G, Scandura JM, Talpaz M, Granacher N, Somervaille TCP, Hoffman R, Wondergem MJ, Salama ME, Colak G, Cui J, Kiladjian JJ, Vannucchi AM, Verstovsek S, Curto-Garcia N, Harrison C, Gupta V. MANIFEST: Pelabresib in Combination With Ruxolitinib for Janus Kinase Inhibitor Treatment-Naive Myelofibrosis. J Clin Oncol. 2023 Nov 10;41(32):4993-5004. doi: 10.1200/JCO.22.01972. Epub 2023 Mar 7.

Reference Type DERIVED
PMID: 36881782 (View on PubMed)

Other Identifiers

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2018-000579-34

Identifier Type: EUDRACT_NUMBER

Identifier Source: secondary_id

CDAK539A12201

Identifier Type: OTHER

Identifier Source: secondary_id

0610-02

Identifier Type: -

Identifier Source: org_study_id

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