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Protocol Details

A Phase I Study to Investigate the Safety of the Ubiquitin Activating Enzyme Inhibitor TAK-243 in Adult Solid Tumor and Lymphoma Patients

This study is currently recruiting participants.

Summary | Eligibility | Citations | Contacts

Summary

Number

001569-C

Sponsoring Institute

National Cancer Institute (NCI)

Recruitment Detail

Type: Participants currently recruited/enrolled
Gender: Male & Female
Min Age: 18 Years
Max Age: 100 Years

Referral Letter Required

No

Population Exclusion(s)

Pregnant Women;
Children

Keywords

Ubiquitin Activating Enzime

Recruitment Keyword(s)

None

Condition(s)

Solid Tumors;
Lymphoma;
Neoplasm

Investigational Drug(s)

TAK-243

Investigational Device(s)

None

Intervention(s)

Drug: TAK-243

Supporting Site

National Cancer Institute

Background:

Certain types of cancer cells are able to divide, grow, and spread quickly. A study drug called ubiquitin-activating enzyme inhibitor (TAK-243) may be able to disrupt this process. TAK-243 may also be able to inhibit the spread of cancer cells without harming healthy cells.

Objective:

To test TAK-243 in people with advanced solid tumors and lymphomas.

Eligibility:

People aged 18 years and older with lymphomas or advanced solid tumors that have grown or spread after treatment.

Design:

Participants will have a physical exam. They will have blood tests and tests of their heart function. They will have imaging scans of their tumors.

TAK-243 is administered through a tube attached to a needle inserted into a vein in the arm (IV infusion). The IV infusion will last 30 minutes.

Participants will be assigned to one of two groups:

Group A will receive TAK-243 twice a week over 21-day cycles.

Group B will receive TAK-243 once a week over 28-day cycles.

Blood tests will be done at every study visit. Additional blood samples will be taken for research. Heart function tests will be repeated on the first day of each cycle.

Participants may remain in the study for as long as their cancer does not get worse and any side effects are tolerable.

If participants stop taking TAK-243, they will be monitored for an additional 3 months.

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Eligibility

INCLUSION CRITERIA:

-Patients with histologically documented advanced or metastatic solid tumors with relapsed or refractory disease who have received standard-of-care or approved therapies known to confer clinical benefit, or patients with aggressive lymphomas who have received >= 2 prior lines of lymphoma-directed therapy and who do not have remaining effective treatment options (including transplant). Additionally, patients with indolent lymphomas must meet criteria for treatment.

-Patients must have measurable or evaluable disease.

-Age >=18 years.

-ECOG performance status <=2.

-Patients must have normal organ and marrow function as defined below:

--hemoglobin

>=9 g/dL (patients may be transfused to achieve this value; elevated indirect bilirubin due to post-transfusion hemolysis is allowed)

--absolute neutrophil count

>=1,000/mcL

--platelets

>=75,000/mcL

--total bilirubin

<=1.5 x institutional upper limit of normal (ULN)

--AST(SGOT)/ALT(SGPT)

<=3 x institutional ULN

OR

<=5 x institutional upper limit of normal for patients with liver metastases at baseline

--creatinine

<=1.5 x institutional ULN

OR

creatinine clearance >=60 mL/min/1.73 m^2 by Cockcroft-Gault

-Any prior therapy must have been completed >= 4 weeks, or >= 5 half-lives of the prior agent (whichever is shorter) prior to enrollment on protocol. Prior definitive radiation should have been completed >= 4 weeks prior to enrollment; prior palliative radiation should have been completed >= 2 weeks prior to enrollment. Patients must be >= 2 weeks since any investigational agent administered as part of a Phase 0 study (where a sub-therapeutic dose of drug is administered) and should have recovered to grade 1 or baseline from any toxicities.

-Female patients who:

--Are postmenopausal (age-related amenorrhea >= 12 consecutive months or follicle-stimulating hormone > 40 mIU/mL), for at least 1 year before the screening visit, OR

--Are surgically sterile (i.e., who had undergone hysterectomy or bilateral oophorectomy), OR

If they are of childbearing potential:

--Agree to practice 1 highly effective method and 1 additional effective (barrier) method of contraception, at the same time, from the time of signing the informed consent through 4 months after the last dose of study drug (female and male condoms should not be used together), or

--Agree to practice true abstinence, when this is in line with the preferred and usual lifestyle of the subject. (Periodic abstinence [e.g., calendar, ovulation, symptothermal, postovulation methods] withdrawal, spermicides only, and lactational amenorrhea are not acceptable methods of contraception.)

-Male patients, even if surgically sterilized (i.e., status postvasectomy), who:

--Agree to practice effective barrier contraception during the entire study treatment period and through 4 months after the last dose of study drug (female and male condoms should not be used together), or

--Agree to practice true abstinence, when this is in line with the preferred and usual lifestyle of the subject. (Periodic abstinence [eg, calendar, ovulation, symptothermal, postovulation methods for the female partner] withdrawal, spermicides only, and lactational amenorrhea are not acceptable methods of contraception.)

The effects of TAK-243 on the developing human fetus are unknown. For this reason and because ubiquitin-activating enzyme inhibitors are known to be teratogenic, women of child-bearing potential and men must agree to use adequate contraception (hormonal or barrier method of birth control; abstinence) prior to study entry and for the duration of study participation. Should a woman become pregnant or suspect she is pregnant while she or her partner is participating in this study, she should inform her treating physician immediately. Men treated or enrolled on this protocol must also agree to use adequate contraception prior to the study, for the duration of study participation, and 4 months after completion of TAK-243 administration.

-Ability to understand and the willingness to sign a written informed consent document.

-Willingness to provide blood for research purposes.

-For expansion phase patients, willingness to undergo 2 core needle biopsy procedures for research purposes if there is a lesion or lesions amenable to repeat biopsy.

-Patients on anticoagulation therapy are eligible for this study in the absence of anticipated drug-drug interactions (DDI) between the

anticoagulation agent and TAK-243. If DDI are anticipated and another anticoagulation agent that is compatible with TAK-243 exists, the patient will be transitioned to this alternative, TAK-243 compatible anticoagulation agent.

EXCLUSION CRITERIA:

-Patients who are receiving any other investigational agents.

-Uncontrolled intercurrent illness including, but not limited to, ongoing or active infection or psychiatric illness/social situations that would limit compliance with study requirements.

-Life-threatening illness unrelated to cancer.

-Patients with uncontrolled coagulopathy or bleeding disorder.

-Known hepatic cirrhosis or severe pre-existing hepatic impairment.

-Known cardiopulmonary disease defined as:

--Unstable angina pectoris;

--Congestive heart failure (New York Heart Association [NYHA] Class III or IV;

--Myocardial infarction (MI) within 6 months prior to first dose (patients who had ischemic heart disease such as a [ACS], MI, and/or revascularization greater than 6 months before screening and who are without cardiac symptoms may enroll);

--Cardiomyopathy.

-Clinically significant arrhythmia:

--History of polymorphic ventricular fibrillation or torsade de pointes,

--Permanent atrial fibrillation (a fib), defined as continuous a fib for >=6 months,

--Persistent a fib, defined as sustained a fib lasting >7 days and/or requiring cardioversion in the 4 weeks before screening,

--Grade 3 a fib defined as symptomatic and incompletely controlled medically, or controlled with device (e.g., pacemaker) or ablation, and

--Patients with paroxysmal a fib or <Grade 3 a fib for period of at least 6 months are permitted to enroll provided that their rate is controlled on a stable regimen.

-Prolonged rate corrected QT (QTc) interval >=470 msec, calculated according to institutional guidelines.

-Uncontrolled high blood pressure (i.e., systolic blood pressure >180 mm Hg, diastolic blood pressure >95 mm Hg).

-Known moderate to severe chronic obstructive pulmonary disease, interstitial lung disease, and pulmonary fibrosis.

-Major surgery within 14 days before the first dose of any study drug.

-Female patients who intend to donate eggs (ova) during the course of this study or 4 months after receiving their last dose of study drug(s).

-Male patients who intend to donate sperm during the course of this study or 4 months after receiving their last dose of study drug(s).

-Patients with known brain metastases or carcinomatous meningitis are excluded from this clinical trial, with the exception of patients whose brain metastatic disease status has remained stable for >= 1 month after treatment of the brain metastases. Patients on anti-seizure medications may be enrolled at the discretion of the Principal Investigator.

-TAK-243 is primarily metabolized by CYP3A4/5. Therefore, the concomitant use of strong inhibitors of CYP3A4/5 (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, indinavir, nelfinavir and saquinavir) and strong inducers of CYP3A4/5 (e.g. rifampin, phenytoin, carbamazepine, phenobarbital, St. John s Wort) is not permitted from 14 days prior to enrollment until the end of the study.

TAK-243 is a substrate for both OATP in human hepatocytes and the drug efflux transporter BCRP (ABCG2). Therefore, concomitant use of drugs that are strong inhibitors of BCRP or OATP is not permitted from 14 days prior to enrollment until the end of the study.

Other medications that are prohibited while on TAK-243 treatment include herbal medications/preparations (except for vitamins). Because the lists of these agents are constantly changing, it is important to regularly consult a frequently-updated medical reference for a list of drugs to avoid or minimize use of.

Patient Drug Information Handout and Wallet Card should be provided to patients. As part of the enrollment/informed consent procedures, the patient will be counseled on the risk of interactions with other agents, and what to do if new medications need to be prescribed or if the patient is considering a new over-the-counter medicine or herbal product.

-Patients undergoing vaccination with live vaccines and live attenuated vaccines in the 30 days prior to receiving TAK-243, during the study, and for 100 days after the last dose of study drug. Inactivated vaccines are permitted.

-History of allergic reactions attributed to compounds of similar chemical or biologic composition to TAK-243.

-Patients with evidence of chronic hepatitis B virus (HBV) infection who are currently on treatment are eligible if they have an undetectable HBV viral load.

-Patients with a history of hepatitis C virus (HCV) infection must have been treated and cured. For patients with HCV infection who are currently on treatment, they are eligible if they have an undetectable HCV viral load.

-Known HIV-positive patients who meet the following criteria will be considered eligible:

--CD4 count > 350 cells/mm3

--Undetectable viral load for 6 months prior to enrollment

--Maintained on modern therapeutic regimens utilizing non-CYP-interactive agents

-Pregnant and lactating/breast-feeding women are excluded from this study because TAK-243 is a UAE-inhibiting agent with the potential for teratogenic or abortifacient effects and there is an unknown but potential risk for adverse events in nursing infants secondary to treatment of the mother with TAK-243.


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Citations:

Hyer ML, Milhollen MA, Ciavarri J, Fleming P, Traore T, Sappal D, Huck J, Shi J, Gavin J, Brownell J, Yang Y, Stringer B, Griffin R, Bruzzese F, Soucy T, Duffy J, Rabino C, Riceberg J, Hoar K, Lublinsky A, Menon S, Sintchak M, Bump N, Pulukuri SM, Langston S, Tirrell S, Kuranda M, Veiby P, Newcomb J, Li P, Wu JT, Powe J, Dick LR, Greenspan P, Galvin K, Manfredi M, Claiborne C, Amidon BS, Bence NF. A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment. Nat Med. 2018 Feb;24(2):186-193. doi: 10.1038/nm.4474. Epub 2018 Jan 15. PMID: 29334375.

Barghout SH, Patel PS, Wang X, Xu GW, Kavanagh S, Halgas O, Zarabi SF, Gronda M, Hurren R, Jeyaraju DV, MacLean N, Brennan S, Hyer ML, Berger A, Traore T, Milhollen M, Smith AC, Minden MD, Pai EF, Hakem R, Schimmer AD. Preclinical evaluation of the selective small-molecule UBA1 inhibitor, TAK-243, in acute myeloid leukemia. Leukemia. 2019 Jan;33(1):37-51. doi: 10.1038/s41375-018-0167-0. Epub 2018 Jun 8. PMID: 29884901.

Murai Y, Jo U, Murai J, Jenkins LM, Huang SN, Chakka S, Chen L, Cheng K, Fukuda S, Takebe N, Pommier Y. SLFN11 Inactivation Induces Proteotoxic Stress and Sensitizes Cancer Cells to Ubiquitin Activating Enzyme Inhibitor TAK-243. Cancer Res. 2021 Jun 1;81(11):3067-3078. doi: 10.1158/0008-5472.CAN-20-2694. Epub 2021 Apr 16. PMID: 33863777; PMCID: PMC8178208.

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Contacts:

Principal Investigator

Referral Contact

For more information:

Sarah J. Shin, M.D.
National Cancer Institute (NCI)
NIHBC 31 BG RM 3A44
31 CENTER DR
BETHESDA MD 20892
(240) 781-4025
sarah.shin@nih.gov

DTC Referral Coordinators
National Cancer Institute (NCI)

(240) 781-3400
dtcreferralcoordinators@nih.gov

NCI Referral Office
National Institute of Health Clinical Center (CC), 9000 Rockville Pike, Bethesda, Maryland 20892, United States: NCI Clinical Trials Referral Office
1-888-NCI-1937
ncimo_referrals@mail.nih.gov

Clinical Trials Number:

NCT06223542

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