A Comparative, Pharmacokinetic Study of CB-839 Capsule and Tablet Formulations in Healthy Adults

NCT02944435 | Completed Phase 1

• 1 other identifier: CX-839-006
• Study Type: interventional
• Target: 14
• Locations: 1 country
• Sites: 1

Brief Summary

This is a Phase 1, randomized, single-dose, 2-way crossover PK comparability study of CB-839 administered as capsule and tablet formulations in healthy adult subjects.

Conditions

Healthy Volunteers

Keywords

Glutaminase Inhibitor; Glutaminase; CB-839

Outcome Measures

Primary Outcomes (6)

• Comparison of Area Under the Curve (AUC) of CB-839 capsules and CB-839 tablets

  To compare the AUC from time zero to the last measurable concentration and from zero to infinity of a single 600 mg dose of CB-839 tablets (Test) and a single 600 mg dose of CB-839 capsules (Reference Treatment)

  -0.5 hr (predose), 0.5, 1, 2, 4, 5, 6, 8, 10, 12 and 24 hours postdose on Day 1 & Day 3

• Comparison of Maximum Concentrations (Cmax) of CB-839 capsules and CB-839 tablets

  To compare the Cmax of a single 600 mg dose of CB-839 tablets (Test) and a single 600 mg dose of CB-839 capsules (Reference Treatment)

  -0.5 hr (predose), 0.5, 1, 2, 4, 5, 6, 8, 10, 12 and 24 hours postdose on Day 1 & Day 3

• Comparison of Time to Observed Maximum Concentrations (Tmax) of CB-839 capsules and CB-839 tablets

  To compare the Tmax of a single 600 mg dose of CB-839 tablets (Test) and a single 600 mg dose of CB-839 capsules (Reference Treatment)

  -0.5 hr (predose), 0.5, 1, 2, 4, 5, 6, 8, 10, 12 and 24 hours postdose on Day 1 & Day 3

• Comparison of the Apparent Terminal Elimination Half-Life of CB-839 capsules and CB-839 tablets

  To compare the apparent terminal elimination half-life of a single 600 mg dose of CB-839 tablets (Test) and a single 600 mg dose of CB-839 capsules (Reference Treatment)

  -0.5 hr (predose), 0.5, 1, 2, 4, 5, 6, 8, 10, 12 and 24 hours postdose on Day 1 & Day 3

• Comparison of the Apparent Terminal Elimination Rate Constant of CB-839 capsules and CB-839 tablets

  To compare the apparent terminal elimination rate constant of a single 600 mg dose of CB-839 tablets (Test) and a single 600 mg dose of CB-839 capsules (Reference Treatment)

  -0.5 hr (predose), 0.5, 1, 2, 4, 5, 6, 8, 10, 12 and 24 hours postdose on Day 1 & Day 3

• The safety of CB-839 capsules and tablets by examining incidence, severity, relationship, type of AE, changes in clinical laboratory tests (hematology, serum chemistry, urinalysis), physical examination, 12-lead ECGs, vital signs and concomitant therapy

  Subjects will be monitored for safety by examining the incidence, severity, relationship, and type of AE as well as changes in clinical laboratory tests (hematology, serum chemistry, urinalysis), physical examination, 12-lead ECGs, vital signs and concomitant therapy.

  8 days

Study Arms (2)

CB-839 Capsules

EXPERIMENTAL

A single dose of 3 x 200-mg capsules of CB-839 will be administered orally with water approximately 5 minutes after consuming an entire meal

Drug: CB-839 Capsules

CB-839 Tablets

ACTIVE COMPARATOR

A single dose of 3 x 200-mg tablets of CB-839 will be administered orally with water approximately 5 minutes after consuming an entire meal

Drug: CB-839 Tablets

Interventions

CB-839 Capsules DRUG

3 x 200 mg CB-839 Capsules (Reference Formulation)

Also known as: Glutaminase inhibitor

CB-839 Capsules

CB-839 Tablets DRUG

3 x 200 mg CB-839 Tablets (Test Formulation)

Also known as: Glutaminase inhibitor

CB-839 Tablets

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy, adult, male or female, 18-55 years of age, inclusive, at screening.
• Has not used nicotine containing products for at least 3 mo prior the first dose.
• Body mass index (BMI) within 18.0 and 30.0 kg/m2, inclusively, at screening.
• Medically healthy with no clinically significant medical history, physical examination, laboratory profiles, vital signs, or ECGs, as deemed by the Principal Investigator (PI).
• For a female of childbearing potential: either be sexually inactive (abstinent) for 14 days prior to the first dose and through 14 days following the last dose of study drug(s) or be using one of the following acceptable birth control methods:
• Non-hormone releasing intrauterine device in place for at least 3 mo prior to the first dose of study drug with either a physical (e.g., condom, diaphragm) or a chemical (e.g., spermicide) barrier method from the time of screening through 14 days following the last dose of study drug.
• A physical barrier method (e.g., condom, diaphragm) with a chemical barrier method (e.g., spermicide) for at least 14 days prior to the first dose of study drug and until 14 days after the last dose of study drug.
• In addition, female subjects of childbearing potential will be advised to remain sexually inactive or to keep the same birth control method or for at least 14 days following the last dose of study drug.
• For a female of non-childbearing potential: must have undergone one of the following sterilization procedures at least 6 mo prior to the first dose of study drug:
• hysteroscopic sterilization;
• bilateral tubal ligation or bilateral salpingectomy;
• non-surgical transcervical sterilization (e.g., Essure®);
• hysterectomy;
• bilateral oophorectomy;
• or be postmenopausal with amenorrhea for at least 1 year prior to the first CB-839 dose with FSH serum levels consistent with postmenopausal status as per PI judgment.

You may not qualify if:

• Subject is mentally or legally incapacitated or has significant emotional problems at the time of the screening visit or is expected to manifest significant emotional problems during the conduct of the study.
• History or presence of clinically significant medical or psychiatric condition or disease in the opinion of the PI.
• History of any illness that, in the opinion of the PI, might confound the results of the study or poses an additional risk to the subject by their participation in the study.
• History or presence of alcoholism or drug abuse within the past 2 years prior to screening.
• History or presence of hypersensitivity or idiosyncratic reaction to the study drugs or inactive ingredient(s).
• History or presence of:
• liver disease, pancreatic insufficiency or intestinal malabsorption;
• neuropathy or muscle disorders;
• seizures;
• asthma;
• fluid retention;
• cardiovascular disease, cardiac arrhythmias, hypertension, cardiovascular thrombotic events, myocardial infarction, or stroke;
• ulcer disease or gastrointestinal bleeding;
• renal papillary necrosis and other renal injury;
• exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis.

Sponsors & Collaborators

• Calithera Biosciences, Inc: lead

Study Sites (1)

Algorithme Pharma USA, LLC

Fargo, North Dakota, 58104, United States

Location

MeSH Terms

Interventions

CB-839

Study Officials

• Jeffery Peterson, MD

  Algorithme Pharma USA LLC

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: October 21, 2016
• First Posted: October 25, 2016
• Study Start: October 1, 2016
• Primary Completion: November 1, 2016
• Study Completion: November 1, 2016
• Last Updated: January 4, 2017

Record last verified: 2017-01

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)