A UGT1A1 Genotype-Directed Study of Belinostat Pharmacokinetics and Toxicity

NCT ID: NCT06406465

Last Updated: 2025-12-26

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

RECRUITING

Clinical Phase

PHASE2

Total Enrollment

60 participants

Study Classification

INTERVENTIONAL

Study Start Date

2025-12-30

Study Completion Date

2028-07-30

Brief Summary

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Background:

High-grade neuroendocrine carcinomas (HGNEC) are cancers that develop in different parts of the body, including the digestive tract, genitals, neck, and head. One drug (belinostat), combined with 2 other drugs (etoposide and cisplatin), is approved to treat HGNEC. But some people may have a gene variant that affects how quickly their body gets rid of the drug; these people may do better with different dosages of belinostat.

Objective:

To test higher or lower doses of belinostat based on gene variants in people with HGNEC.

Eligibility:

People aged 18 years and older with HGNEC.

Design:

Participants will be screened. They will have a physical exam with blood tests. Some blood will be used for genetic testing. They will have imaging scans and a test of their heart function. Samples of tumor tissue may be collected.

All 3 study drugs (belinostat, etoposide, cisplatin) are given through a tube attached to a needle inserted into a vein. Treatment will be given in 21-day cycles.

For cycles 1 through 6: Participants will come to the clinic for the first 4 days. They will be given all 3 drugs. Imaging scans and other tests will be repeated. Each visit will last 4 to 8 hours.

After cycle 6: Participants may continue treatment with belinostat alone. They will come to the clinic for the first 3 days of each cycle. They may continue treatment for up to 5 years if the drug is helping them.

Participants will have a follow-up visit 30 days after their last dose of belinostat. Then they will receive follow-up visits by phone or email every 3 to 6 months.

Detailed Description

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Background:

* Extrapulmonary High-Grade Neuroendocrine Neoplasms (HGNENs) are all high-grade neoplasms that may resemble small cell carcinoma or large cell Neuroendocrine Carcinomas (NEC) of the lung. Poorly differentiated NECs are often associated with a rapidly progressive disease and a proliferative rate (Ki67%) \>20%.
* As a general rule, poorly differentiated NECs are treated with platinum-based regimens according to small cell carcinoma guidelines.
* This protocol will study a continuous infusion of the histone deacetylase (HDAC) inhibitor belinostat in combination with cisplatin and etoposide for patients with advanced neuroendocrine neoplasms.

Objective:

-To determine if pharmacogenomic intervention can normalize the area under the curve (AUC) at cycle 6 between UGT1A1\*28 and UGT1A1\*60 genotypes) of belinostat administered as a continuous 48 h infusion in combination with cisplatin and etoposide in participants with neuroendocrine malignancies based on UGT1A1\*28 and UGT1A1\*60 genotypes.

Eligibility:

* The protocol will be open to participants with Extrapulmonary High-Grade Neuroendocrine Neoplasms (HGNENs)
* Participants will be recruited based on genotype, with n=9 carrying UGT1A1\*1/\*1 or UGT1A1\*1/\*28 and n=30 carrying any other combination of variant alleles at UGT1A1\*28 or UGT1A1\*60.
* Age \>=18 years
* ECOG Performance Status 0-2

Design:

* Parallel design in which the starting dose of belinostat is administered as a 48-hour continuous infusion at two possible doses based on genotype: 1) 400mg/m\^2/day for UGT1A1\*28/\*28 or at least one UGT1A1\*60 allele UGT1A1\*28 and UGT1A1\*60 genotypes or 2) 600 mg/m\^2/day for wild-type participants and those carrying UGT1A1\*1/\*28 in the absence of other variant alleles.
* To define pharmacokinetics, toxicities of belinostat provided to participants who carry the above genotype groups.
* All participants will also receive cisplatin at 60 mg/m\^2 IV on day 2, and etoposide at 80 mg/m\^2 IV daily x3 on days 2 - 4.

Conditions

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Carcinoma, Neuroendocrine Tumor, Neuroendocrine Tumors, Neuroendocrine Neuroendocrine; Carcinoma Small Cell; Receptors

Keywords

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High-grade carcinomas Resemble small cell carcinoma Large cell NEC Histone Deacetylase Genotypes Neuroendocrine malignancies

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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Arm 1

Belinostat at 400 mg/m\^2/day plus Cisplatin plus Etoposide

Group Type EXPERIMENTAL

Belinostat

Intervention Type DRUG

400mg/m\^2/24h or 600 mg/m\^2/24h IV over (48h continuous infusion) on days 1, 2 and 3 based on UGT1A1 status

Cisplatin

Intervention Type DRUG

60 mg/m\^2 IV over 60 minutes on day 2

Etoposide

Intervention Type DRUG

80 mg/m\^2 IV over 60 minutes on day 2 after infusion of cisplatin and again on days 3 and 4

Arm 2

Belinostat at 600 mg/m\^2/day plus Cisplatin plus Etoposide

Group Type EXPERIMENTAL

Belinostat

Intervention Type DRUG

400mg/m\^2/24h or 600 mg/m\^2/24h IV over (48h continuous infusion) on days 1, 2 and 3 based on UGT1A1 status

Cisplatin

Intervention Type DRUG

60 mg/m\^2 IV over 60 minutes on day 2

Etoposide

Intervention Type DRUG

80 mg/m\^2 IV over 60 minutes on day 2 after infusion of cisplatin and again on days 3 and 4

Interventions

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Belinostat

400mg/m\^2/24h or 600 mg/m\^2/24h IV over (48h continuous infusion) on days 1, 2 and 3 based on UGT1A1 status

Intervention Type DRUG

Cisplatin

60 mg/m\^2 IV over 60 minutes on day 2

Intervention Type DRUG

Etoposide

80 mg/m\^2 IV over 60 minutes on day 2 after infusion of cisplatin and again on days 3 and 4

Intervention Type DRUG

Eligibility Criteria

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Inclusion Criteria

1. Participants must have histologically confirmed diagnosis of Extrapulmonary High-Grade Neuroendocrine Neoplasms (HGNENs) for which there is no known standard therapy capable of extending life expectancy.
2. Age \>= 18 years.
3. Participants with neuroendocrine prostate cancer may continue ongoing LHRH agonist therapy.
4. Participants with bone metastases or hypercalcemia who began intravenous bisphosphonate treatment prior to study entry may continue this treatment while on study.
5. Evaluable (measurable or non-measurable) disease, per RECIST 1.1.
6. ECOG performance status \<=2 at screening
7. Participants must have adequate organ and marrow function as defined below:

* Leukocytes \>=3,000/mcL
* Hemoglobin \>= 10 g/dL
* Absolute neutrophil count (ANC) \>=1,500/mcL
* Platelets \>=100,000/mcL
* Aspartate aminotransferase (AST) or serum glutamic-oxaloacetic transaminase (SGOT) / Alanine aminotransferase (ALT) or serum glutamic-pyruvic transaminase (SGPT): \<=3 X institutional upper limit of normal
* Total bilirubin \<= 1.5 x institutional upper limit of normal (ULN).

NOTE: In participants with Gilbert s syndrome, a total bilirubin \<= 3.0 X ULN is allowed
* Serum Creatinine \<= 1.5 X institutional ULN OR
* An estimated Creatinine clearance (CrCL) \>=60 mL/min/1.73 m\^2 based on the Cockcroft Gault equation
* Prothrombin time (PT) / International normalized ratio (INR) and Partial thromboplastin time (PTT) \<= 1 X institutional ULN
8. Hepatitis B virus (HBV)-infected participants can be enrolled if HBV DNA is undetectable. Hepatitis C virus (HCV)-infected participants can be enrolled if HCV RNA level is undetectable
9. Women of child-bearing potential (WOCBP) must agree to use effective contraception (hormonal, intrauterine device (IUD), tube ligation, a partner has had a previous vasectomy, abstinence) prior to study entry, during the study, and for 14 months for women after the last dose of the study drug(s). Men with partners of childbearing potential must agree to use effective contraception (abstinence, condoms, previous vasectomy) or request partners to use effective contraception (per above) during the study and for 11 months after the last dose of study therapy.
10. Breastfeeding participants must be willing to discontinue breastfeeding starting with prior to study entry, during the study, and for 3 months after the last dose of the study drug(s).
11. Willing to comply with study procedures and follow-up.
12. Participants must be able to understand and be willing to sign a written informed consent document.

Exclusion Criteria

1. Participants with prior investigational drug, chemotherapy, immunotherapy or any prior radiotherapy (except for palliative bone directed therapy) within the past 14 days prior to the first drug administration. Additionally, FDA-approved hormonal therapy for the treatment or prevention of other malignancies (e.g., breast cancer, prostate cancer) may be continued where in the opinion of the investigator stopping such therapies may increase the risk of disease progression. Potential drug-drug interactions with the hormonal agent will be assessed by the investigator prior to enrollment.
2. History of allergic reactions attributed to compounds of similar chemical or biologic composition to belinostat, cisplatin, etoposide or other agents used in study. Participants with a history of allergic reactions to medications containing polysorbate 80 will be evaluated on a case-by-case basis.
3. Participants with treated brain metastases are not eligible except if follow-up brain imaging after central nervous system (CNS)-directed therapy shows no evidence of progression.
4. Participants who have not recovered (CTCAE \<= grade 1) from non heme adverse events due to prior treatments, except for alopecia, or stable grade 2 tinnitus (not interfering with ADL's) or baseline hearing loss by audiometry or stable grade 2 sensory neuropathy (moderate symptoms; limiting instrumental ADL) without pain or motor component, and not interfering with ADL's.
5. Participants taking strong UGT1A1 inhibitors or CYP3A4 inhibitors or inducers must discontinue their use a minimum of 5 half-lives prior to starting treatment on this trial
6. Participants with platinum-refractory disease.
7. Participants who have had another histone deacetylase inhibitor (e.g., valproic acid, vorinostat) for at least 2 weeks prior to enrollment.
8. Participants who have had radiation to the pelvis or other bone marrow-bearing sites will be considered on a case-by-case basis and may be excluded if the bone marrow reserve is not considered adequate (\>25% of bone marrow).
9. Pregnancy (confirmed with beta-Human chorionic gonadotropin (HCG) serum or urine pregnancy test performed in WOCBP at screening)
10. Significant cardiovascular disease (New York Heart Association Class III or IV cardiac disease), myocardial infarction within the past 6 months, unstable angina, unstable arrhythmia, or a need for anti-arrhythmic therapy (use of medication to control heart rate in participants with atrial fibrillation is allowed, if stable medication for at least last month prior to enrollment and medication not listed as causing Torsade de Points), or evidence of acute ischemia on ECG.
11. Baseline prolongation of QT/QTc interval, i.e., defined as an average QTc interval \> 450 msec calculated using the Fridericia formula for QT correction; Long QT Syndrome; or the required use of concomitant medication that may cause Torsade de Pointes.
12. Participants with HIV infection if CD4 count \<200 cells per cubic millimeter before treatment initiation
13. Uncontrolled intercurrent illness that would limit compliance with study requirements.
Minimum Eligible Age

18 Years

Maximum Eligible Age

120 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

No

Sponsors

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National Cancer Institute (NCI)

NIH

Sponsor Role lead

Responsible Party

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Responsibility Role SPONSOR

Principal Investigators

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Jaydira Del Rivero, M.D.

Role: PRINCIPAL_INVESTIGATOR

National Cancer Institute (NCI)

Locations

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National Institutes of Health Clinical Center

Bethesda, Maryland, United States

Site Status RECRUITING

Countries

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United States

Central Contacts

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Anna Liza F Rivero

Role: CONTACT

Phone: (240) 858-7946

Email: [email protected]

Jaydira Del Rivero, M.D.

Role: CONTACT

Phone: (240) 858-3851

Email: [email protected]

Facility Contacts

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Anna Rivero

Role: primary

NCI Medical Oncology Referral Office

Role: backup

Related Links

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Other Identifiers

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001601-C

Identifier Type: -

Identifier Source: secondary_id

10001601

Identifier Type: -

Identifier Source: org_study_id