---
title: Palbociclib Pharmacokinetics Study In Postmenopausal Chinese Women With ER (+), HER2 (-) Advanced Breast Cancer
nct_id: NCT02499146
overall_status: COMPLETED
phase: PHASE1
sponsor: Pfizer
study_type: INTERVENTIONAL
primary_condition: Advanced Breast Cancer
countries: China
canonical_url: "https://parkinsonspathways.com/agent/trials/NCT02499146.md"
clinicaltrials_gov: "https://clinicaltrials.gov/study/NCT02499146"
ct_last_update_post_date: 2026-02-11
last_seen_at: "2026-05-12T07:00:58.985Z"
source: ClinicalTrials.gov (mirrored, no enrichment)
---
# Palbociclib Pharmacokinetics Study In Postmenopausal Chinese Women With ER (+), HER2 (-) Advanced Breast Cancer

**Official Title:** A PHASE 1 OPEN-LABEL PHARMACOKINETICS STUDY OF PALBOCICLIB, A CYCLIN-DEPENDENT KINASE 4 AND 6 (CDK4/6) INHIBITOR, IN POSTMENOPAUSAL CHINESE WOMEN WITH ER (+), HER2 (-) ADVANCED BREAST CANCER

**NCT ID:** [NCT02499146](https://clinicaltrials.gov/study/NCT02499146)

## Key Facts

- **Status:** COMPLETED
- **Phase:** PHASE1
- **Study Type:** INTERVENTIONAL
- **Target Enrollment:** 26
- **Lead Sponsor:** Pfizer
- **Conditions:** Advanced Breast Cancer
- **Start Date:** 2015-09-11
- **Completion Date:** 2024-12-24
- **CT.gov Last Update:** 2026-02-11

## Brief Summary

As part of the global clinical development program for Palbociclib, studies are planned in cancer patients in China. An assessment of Palbociclib pharmacokinetics in Chinese patients, as required by the Chinese Health Authorities, is therefore warranted. In addition, safety and efficacy will be also evaluated.

The single and multiple 125 mg oral dose pharmacokinetics of Palbociclib will be characterized.

## Eligibility

- **Minimum age:** 18 Years
- **Maximum age:** 65 Years
- **Sex:** FEMALE
- **Healthy Volunteers:** No

```
Inclusion Criteria:

* ER(+), HER2(-), postmenopausal adult (ages 18-65 years, inclusive) Chinese women with proven diagnosis of adenocarcinoma of the breast with evidence locoregionally recurrent or metastatic disease not amenable to resection or radiation therapy with curative intent and for whom chemotherapy is not clinically indicated.

  a. Postmenopausal women: i. Prior bilateral surgical oophorectomy; or ii. Medically confirmed post-menopausal status defined as spontaneous cessation of regular menses for at least 12 consecutive months with no alternative pathological or physiological cause b. Documentation of histologically or cytologically confirmed diagnosis of: i. ER(+) breast cancer. c. Documentation of HER2(-) breast cancer. d. Previously untreated with any systemic anti cancer therapy for their locoregionally recurrent or metastatic ER+ disease.
* Measurable disease as defined per RECIST v.1.1 or bone-only disease. - Tumor lesions previously irradiated or subjected to other locoregional therapy will only be deemed measurable if disease progression at the treated site after completion of therapy is clearly documented.

Exclusion Criteria:

* HER2-positive tumor as defined by documentation of erbB-2 gene amplification by FISH (as defined by a HER2/CEP17 ratio ≥2) or chromogenic in situ hybridization (CISH, as defined by the manufacturer's kit instruction) or documentation of HER2 overexpression by IHC (defined as IHC3+, or IHC2+ with FISH or CISH confirmation) based on local laboratory results
* Patients with advanced, symptomatic, visceral spread, that are at risk of life-threatening complications in the short term (including patients with massive uncontrolled effusions \[pleural, pericardial, peritoneal\], pulmonary lymphangitis, and over 50% liver involvement).
```

## Arms

- **Cohort 1** (EXPERIMENTAL) — Combination therapy of palbociclib and letrozole

## Interventions

- **Palbociclib** (DRUG) — 125 mg orally once daily with food on Day 1 to Day 21 followed by 7 days off treatment in a 28-day cycle
- **Letrozole** (DRUG) — 2.5 mg , orally once daily (continuously)

## Primary Outcomes

- **Single-dose Pharmacokinetics (PK): Maximum Plasma Concentration (Cmax) for Palbociclib** _(time frame: Lead-in phase: Day 1 pre-dose, 2, 4, 6, 8, 10, 24, 48, 72, 96 and 120 hours post dose)_ — Cmax of palbociclib in the single-dose part (lead-in phase) was observed directly from data.
- **Single-dose PK: Time to Reach Maximum Plasma Concentration (Tmax) for Palbociclib** _(time frame: Lead-in phase: Day 1 pre-dose, 2, 4, 6, 8, 10, 24, 48, 72, 96 and 120 hours post dose)_ — Tmax for palbociclib in the single-dose part (lead-in phase) was observed directly from data as time of first occurrence.
- **Single-dose PK: Area Under the Plasma Concentration Versus Time Curve (AUC) From Time 0 to the Time 10 Hours (AUC10) for Palbociclib** _(time frame: Lead-in phase: Day 1 pre-dose, 2, 4, 6, 8, and 10 hours post dose)_ — AUC10 for palbociclib in the single-dose part (lead-in phase) was obtained by linear/log trapezoidal method.
- **Single-dose PK: AUC From Time 0 to the Time 24 Hours (AUC24) for Palbociclib** _(time frame: Lead-in phase: Day 1 pre-dose, 2, 4, 6, 8, 10, and 24 hours post dose)_ — AUC24 is AUCtau, where the dosing interval (tau) is 24 hours. AUC24 in the single-dose part (lead-in phase) for palbociclib was obtained by linear/log trapezoidal method.
- **Single-dose PK: AUC From Time 0 to the Time of Last Quantifiable Concentration (AUClast) for Palbociclib** _(time frame: Lead-in phase: Day 1 pre-dose, 2, 4, 6, 8, 10, 24, 48, 72, 96 and 120 hours post dose)_ — AUClast for palbociclib in the single-dose part (lead-in phase) was obtained by linear/log trapezoidal method.
- **Single-dose PK: AUC From Time 0 Extrapolated to Infinite Time (AUCinf) for Palbociclib** _(time frame: Lead-in phase: Day 1 pre-dose, 2, 4, 6, 8, 10, 24, 48, 72, 96 and 120 hours post dose)_ — AUCinf for palbociclib in the single-dose part (lead-in phase) was calculated as AUClast + (Clast/kel), where Clast was the predicted plasma concentration at the last quantifiable time point estimated from the log-linear regression analysis and kel was the rate constant for terminal phase obtained by linear regression of the log-linear concentration-time curve.
- **Single-dose PK: Rate Constant for Terminal Phase (Kel) for Palbociclib** _(time frame: Lead-in phase: Day 1 pre-dose, 2, 4, 6, 8, 10, 24, 48, 72, 96 and 120 hours post dose)_ — Kel for palbociclib in the single-dose part (lead-in phase) was obtained by linear regression of the log-linear concentration-time curve.
- **Single-dose PK: Mean Residence Time (MRT) for Palbociclib** _(time frame: Lead-in phase: Day 1 pre-dose, 2, 4, 6, 8, 10, 24, 48, 72, 96 and 120 hours post dose)_ — MRT for palbociclib in the single-dose part (lead-in phase) was calculated as AUMCinf/AUCinf, where AUMCinf was area under the first moment curve from time 0 to infinity.
- **Single-dose PK: Terminal Half-Life (t1/2) for Palbociclib** _(time frame: Lead-in phase: Day 1 pre-dose, 2, 4, 6, 8, 10, 24, 48, 72, 96 and 120 hours post dose)_ — t1/2 for palbociclib in the single-dose part (lead-in phase) was calculated as Loge(2)/kel.
- **Single-dose PK: Apparent Oral Clearance (CL/F) for Palbociclib** _(time frame: Lead-in phase: Day 1 pre-dose, 2, 4, 6, 8, 10, 24, 48, 72, 96 and 120 hours post dose)_ — CL/F for palbociclib in the single-dose part (lead-in phase) was calculated as Dose/AUCinf.
- **Single-dose PK: Apparent Volume of Distribution (Vz/F) for Palbociclib** _(time frame: Lead-in phase: Day 1 pre-dose, 2, 4, 6, 8, 10, 24, 48, 72, 96 and 120 hours post dose)_ — Vz/F for palbociclib in the single-dose part (lead-in phase) was calculated as Dose/(AUCinf \* kel).
- **Multiple-dose PK: Maximum Plasma Concentration at Steady State (Css,Max) for Palbociclib** _(time frame: Cycle 1: pre-dose on Day 19, Day 20, Day 21, and 2, 4, 6, 8, 10, 24, 48, 72, 96, 120 hours post dose on Day 21)_ — Css,max of palbociclib in the multiple-dose part (Cycle 1) was observed directly from data.
- **Multiple-dose PK: Minimum Plasma Concentration at Steady State (Css,Min) for Palbociclib** _(time frame: Cycle 1: pre-dose on Day 19, Day 20, Day 21, and 2, 4, 6, 8, 10, 24, 48, 72, 96, 120 hours post dose on Day 21)_ — Css,min of palbociclib in the multiple-dose part (Cycle 1) was observed directly from data.
- **Multiple-dose PK: AUC Within a Dosing Interval of Tau (=24 Hours) at Steady State (AUCss,Tau) for Palbociclib** _(time frame: Cycle 1: pre-dose on Day 19, Day 20, Day 21, and 2, 4, 6, 8, 10, and 24 hours post dose on Day 21)_ — AUCss,tau of palbociclib in the multiple-dose part (Cycle 1) was determined by linear/log trapezoidal method.
- **Multiple-dose PK: Average Plasma Concentration at Steady State (Css,av) for Palbociclib** _(time frame: Cycle 1: pre-dose on Day 19, Day 20, Day 21, and 2, 4, 6, 8, 10, and 24 hours post dose on Day 21)_ — Css,av of palbociclib in the multiple-dose part (Cycle 1) was calculated as AUCss,tau/tau, where tau was 24 hours.
- **Multiple-dose PK: Time to Reach Maximum Plasma Concentration at Steady State (Tss,Max) for Palbociclib** _(time frame: Cycle 1: pre-dose on Day 19, Day 20, Day 21, and 2, 4, 6, 8, 10, and 24 hours post dose on Day 21)_ — Tss,max of palbociclib in the multiple-dose part (Cycle 1) was observed directly from data as time of first occurrence within tau (=24 hours) at steady state.
- **Multiple-dose PK: Vz/F for Palbociclib** _(time frame: Cycle 1: pre-dose on Day 19, Day 20, Day 21, and 2, 4, 6, 8, 10, 24, 48, 72, 96, 120 hours post dose on Day 21)_ — Vz/F of palbociclib in the multiple-dose part (Cycle 1) was calculated as Dose/(AUCss,tau \* kel), where AUCss,tau was the AUC within a dosing interval of tau (=24 hours) at steady state and kel was the terminal phase rate constant following multiple-dose calculated by a linear regression of the log-linear concentration-time curve.
- **Multiple-dose PK: t1/2 for Palbociclib** _(time frame: Cycle 1: pre-dose on Day 19, Day 20, Day 21, and 2, 4, 6, 8, 10, 24, 48, 72, 96, 120 hours post dose on Day 21)_ — t1/2 of palbociclib in the multiple-dose part (Cycle 1) was calculated as ln (2)/kel, where kel was the terminal phase rate constant following multiple-dose calculated by a linear regression of the log-linear concentration-time curve.
- **Multiple-dose PK: CL/F for Palbociclib** _(time frame: Cycle 1: pre-dose on Day 19, Day 20, Day 21, and 2, 4, 6, 8, 10, and 24 hours post dose on Day 21)_ — CL/F of palbociclib in the multiple-dose part (Cycle 1) was calculated as Dose/AUCss,tau, where AUCss,tau was the AUC within a dosing interval of tau (=24 hours) at steady state.
- **Multiple-dose PK: Peak to Trough Fluctuation at Steady State (PTF) for Palbociclib** _(time frame: Cycle 1: pre-dose on Day 19, Day 20, Day 21, and 2, 4, 6, 8, 10, 24, 48, 72, 96, 120 hours post dose on Day 21)_ — PTF of palbociclib in the multiple-dose part (Cycle 1) was determined as (Css,max - Css,min)/Css,av. Css,max and Css,min were observed directly from data while Css,av was calculated as AUCss,tau/tau, where tau was 24 hours.
- **Observed Accumulation Ratio (Rac) for Palbociclib** _(time frame: Lead-in phase: Day 1 pre-dose, 2, 4, 6, 8, 10, and 24 hours post dose; Cycle 1: pre-dose on Day 19, Day 20, Day 21, and 2, 4, 6, 8, 10, and 24 hours post dose on Day 21)_ — Rac of palbociclib was determined as AUCss,tau/AUCsd,tau, where AUCss,tau (tau=24 hours) was from multiple-dose part (Cycle 1) and AUCsd,tau was AUC24 from single-dose part (lead-in phase).
- **Steady State Accumulation Ratio (Rss) for Palbociclib** _(time frame: Lead-in phase: Day 1 pre-dose, 2, 4, 6, 8, 10, 24, 48, 72, 96 and 120 hours post dose; Cycle 1: pre-dose on Day 19, Day 20, Day 21, and 2, 4, 6, 8, 10, 24 hours post dose on Day 21)_ — Rss of palbociclib was calculated as AUCss,tau/AUCinf, where AUCss,tau (tau=24 hours) was from multiple-dose part (Cycle 1) and AUCinf was from single-dose part (lead-in phase).

## Secondary Outcomes

- **Number of Participants With Treatment-Emergent Adverse Events (AEs) and Serious Adverse Events (SAEs)** _(time frame: From first dose of study medication up to 28 days after last dose of study medication (up to maximum of 475 weeks, maximum treatment exposure = 471 weeks))_
- **Number of Participants With Treatment-Emergent AEs by Maximum National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) Grade** _(time frame: From first dose of study medication up to 28 days after last dose of study medication (up to maximum of 475 weeks, maximum treatment exposure = 471 weeks))_
- **Number of Participants With Laboratory Test Abnormalities** _(time frame: From first dose of study medication up to 28 days after last dose of study medication (up to maximum of 475 weeks, maximum treatment exposure = 471 weeks))_
- **Number of Participants Meeting the Categorical Summarization Criteria for QTcF and QTcB Parameters** _(time frame: From first dose of study medication up to 28 days after last dose of study medication (up to maximum of 475 weeks, maximum treatment exposure = 471 weeks))_
- **Progression-Free Survival (PFS)** _(time frame: From C1D1 to date of first documentation of PD or death due to any cause, whichever occurred first (up to maximum of 471 weeks of treatment exposure))_
- **Percentage of Participants Achieving Objective Response (Objective Response Rate [ORR])** _(time frame: From C1D1 until disease progression or death due to any cause, whichever occurred first (up to maximum of 471 weeks of treatment exposure))_
- **Percentage of Participants Achieving Disease Control (Disease Control Rate [DCR])** _(time frame: From C1D1 until disease progression or death due to any cause, whichever occurred first (up to maximum of 471 weeks of treatment exposure))_
- **Duration of Response** _(time frame: From first documentation of CR or PR to date of first documentation of objective progression or death, whichever occurred first (up to maximum of 471 weeks of treatment exposure))_
- **1-Year PFS Probability** _(time frame: 1 year)_
- **Trough Plasma Concentration of Letrozole** _(time frame: pre-dose of Cycle 1 Days 19, 20, 21 and Cycle 2 Day 1)_
- **Ratio Over Baseline for Skin Biomarker Phosphorylated Retinoblastoma Protein (pRb) Expression** _(time frame: Baseline (Day -1), lead-in phase Days 1 and 2, Cycle 1 Days 21, 22, 23, 24, 25, 26)_
- **Ratio Over Baseline for Skin Biomarker Ki67 Expression** _(time frame: Baseline (Day -1), lead-in phase Days 1 and 2, Cycle 1 Days 21, 22, 23, 24, 25, 26)_
- **Ratio Over Baseline for Thymidine Kinase (TK) Concentration** _(time frame: Baseline (Day -1 pre-dose), lead-in phase Day 1 (4, 8, 10, 24, 72, 120 hours post dose), Cycle 1 Day 21 (4, 8, 10, 24, 72, 96, 120 hours post dose), Cycle 2 Day 1 pre-dose)_

## Locations (7)

- Beijing Cancer Hospital/Oncology department, Beijing, Beijing Municipality, China
- Sun Yat-Sen University Cancer Center, Guangzhou, Guangdong, China
- Guangdong General Hospital/Department of Breast Surgery, Guangzhou, Guangdong, China
- Harbin Medical University Cancer Hospital, Harbin, Heilongjiang, China
- The first hospital of jilin university, Changchun, Jilin, China
- The First Affiliated Hospital of College of Medicine, Zhejiang University, Hangzhou, Zhejiang, China
- Cancer Institute and Hospital, Chinese Academy of Medical Sciences, Beijing, China

## Recent Field Changes (last 30 days)

- `status.overallStatus` — added _(2026-05-12)_
- `status.primaryCompletionDate` — added _(2026-05-12)_
- `status.completionDate` — added _(2026-05-12)_
- `status.lastUpdatePostDate` — added _(2026-05-12)_
- `design.phases` — added _(2026-05-12)_
- `design.enrollmentCount` — added _(2026-05-12)_
- `eligibility.criteria` — added _(2026-05-12)_
- `eligibility.minAge` — added _(2026-05-12)_
- `eligibility.maxAge` — added _(2026-05-12)_
- `eligibility.sex` — added _(2026-05-12)_
- `outcomes.primary` — added _(2026-05-12)_
- `outcomes.secondary` — added _(2026-05-12)_
- `armsInterventions.arms` — added _(2026-05-12)_
- `armsInterventions.interventions` — added _(2026-05-12)_
- `sponsor.lead` — added _(2026-05-12)_
- `results.hasResults` — added _(2026-05-12)_
- `locations.beijing cancer hospital/oncology department|beijing|beijing municipality|china` — added _(2026-05-12)_
- `locations.sun yat-sen university cancer center|guangzhou|guangdong|china` — added _(2026-05-12)_
- `locations.guangdong general hospital/department of breast surgery|guangzhou|guangdong|china` — added _(2026-05-12)_
- `locations.harbin medical university cancer hospital|harbin|heilongjiang|china` — added _(2026-05-12)_
- `locations.the first hospital of jilin university|changchun|jilin|china` — added _(2026-05-12)_
- `locations.the first affiliated hospital of college of medicine, zhejiang university|hangzhou|zhejiang|china` — added _(2026-05-12)_
- `locations.cancer institute and hospital, chinese academy of medical sciences|beijing||china` — added _(2026-05-12)_

---

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