Study to Investigate the Effect of Formulation and Food on the Pharmacokinetics of GDC-0810

Genentech

Status and phase: Completed; Phase 1

Conditions: Healthy Volunteer

Treatments: Drug: GDC-0810 Phase III Prototype Tablet; Drug: GDC-0810 Phase II Tablet

Study type: Interventional

Funder types: Industry

Identifiers

NCT02722018

GP29826

2015-003730-27 (EudraCT Number)

Details and patient eligibility

About

This is a phase 1, randomized, open-label, single center, crossover study to investigate the effect of formulation and food on the pharmacokinetics of GDC-0810 in female healthy participants of non-childbearing potential. This study is divided into three parts. Participants in each part will be randomized to one of three treatment sequences. Part 1 study in 4 periods will investigate the effect of formulation on the pharmacokinetics (PK) of GDC-0810 administered with low-fat food. Each participant in this part will receive a single dose of GDC-0810 dose level A following consumption of a low fat meal (30 minutes after the start of the meal) in each treatment period. Part 2 is an optional Phase I study in 3 periods to investigate the effect of formulation on the PK of GDC-0810 administered with low-fat food in healthy female participants of non-childbearing potential. Part 3 study in three periods will compare the PK of a Phase III prototype tablet formulation selected from Parts 1 and 2 of the study with the Phase II tablet formulation (both administered 30 minutes after the start of a low fat meal) at dose level B and to investigate the PK of the Phase III prototype formulation administered in the fasted state.

Enrollment: 45 patients

Sex: Female

Ages: 40 to 70 years old

Volunteers: Accepts Healthy Volunteers

Inclusion criteria

• Female participants of non-childbearing potential including non-pregnant, non-lactating, and either postmenopausal or surgically sterile for at least 45 days post procedure
• Body mass index (BMI) range 18.0 to 32.0 kilograms per square meter (kg/m^2), inclusive
• In good health, as determined by no clinically significant findings from medical history, physical examination, 12-lead electrocardiogram (ECG), vital signs, and clinical laboratory evaluations
• Receive an explanation of the mandatory pharmacogenomics (PgX) component of the study

Exclusion criteria

• Any history of endometrial polyps, endometrial cancer, atypical endometrial hyperplasia, or other endometrial disorders unless subjects have undergone total hysterectomy and there is no evidence of active disease
• Significant history or clinical manifestation of any significant metabolic, allergic, dermatological, hepatic, renal, hematological, pulmonary, cardiovascular, gastrointestinal, neurological, or psychiatric disorder
• History of any thrombophilic condition, inflammatory bowel disease, active bowel inflammation, chronic diarrhea, short bowel syndrome, and upper gastro-intestinal (GI) surgery including gastric resection
• Any history of venous thrombosis (including pulmonary embolism [PE])
• Participation in any other investigational study drug trial in which receipt of an investigational study drug occurred within 90 days prior to Check-in (Day -1) in Period 1
• Use of systemic hormone replacement therapy within 1 year prior to Check-in (Day -1)
• History of use of tamoxifen, aromatase inhibitors, or any other endocrine agent for the treatment of breast cancer

Trial design

Primary purpose: Treatment

Allocation: Randomized

Interventional model: Crossover Assignment

Masking: None (Open label)

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45 participants in 3 patient groups

Part 1: GDC-0810 dose level A - Low Fat Meal

Experimental group

Description:

Participants will receive a single dose of GDC-0810 dose level A on Day 1 of each treatment period. GDC-0810 will be administered with low fat meal in the form of Phase II tablet or one of three Phase III prototype tablets (Prototype 1, 2 or 3) in a crossover fashion.

Treatment:

Drug: GDC-0810 Phase III Prototype Tablet

Drug: GDC-0810 Phase II Tablet

Part 2 (Optional): GDC-0810 dose level A - Low Fat Meal

Experimental group

Description:

Participants will receive a single dose of GDC-0810 dose level A on Day 1 of each treatment period. GDC-0810 will be administered with low fat meal in the form of Phase II tablet or one of two Phase III prototype tablets (Prototype 4 or 5) in a crossover fashion.

Treatment:

Drug: GDC-0810 Phase III Prototype Tablet

Drug: GDC-0810 Phase II Tablet

Part 3: GDC-0810 dose level B - Low Fat Meal/Fasted

Experimental group

Description:

Participants will receive a single dose of GDC-0810 dose level B on Day 1 of each treatment period. GDC-0810 will be administered with low fat meal or under fasted condition either as Phase II tablet (with low fat meal) or as the Phase III prototype tablet selected from Parts 1 or 2 (with low fat meal or under fasted conditions), in a crossover fashion.

Treatment:

Drug: GDC-0810 Phase III Prototype Tablet

Drug: GDC-0810 Phase II Tablet