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This study will assess alternative formulations of lapatinib for relative bioavailability and bioequivalence (BE) with the current commercial formulation (reference). Subjects will be dosed for at least one week (7 days) on each formulation and PK samples will be collected after each lapatinib formulation dosing Period on Period 1 Day 7 and Period 2 Day7 at pre-dose and up to 24 hrs post dose. The study may evaluate up to three alternative test formulations. After subjects complete the PK evaluation at the End of Study Visit, if they are eligible, they will have the option to enter EGF111767, an open-label, Phase Ib continuation study of lapatinib monotherapy or lapatinib in combination with other anti-cancer treatments.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Part 1-3 | Experimental | 2-period crossover, Period 1 (D1-7) will receive either the commercial formulation or the alternative formulation. Period 2 (D1-7) will receive the formulation not received in Period 1. There will be 3 parts with 3 different alternative formulations. Subjects will only participate in one part. |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| lapatinib | Drug | 1250 mg or 1500 mg lapatinib commercial tablet |
|
| Measure | Description | Time Frame |
|---|---|---|
| The primary PK endpoints will be AUC(0-24) and Cmax of lapatinib | Period 1 Day 7 and Period 2 Day 7 |
| Measure | Description | Time Frame |
|---|---|---|
| The secondary PK endpoints will be Cmin, tmax, and tlag of lapatinib | Period 1 Day 7 and Period 2 Day 7 | |
| Safety and tolerability endpoints will consist of adverse events and changes in laboratory values. | 2 wks |
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Inclusion Criteria:
NOTE: If subject has a current or recent (within 14 days) history of nausea or emesis, the subject must be reviewed by the Investigator and the GSK medical monitor. Prophylactic antiemetic therapy may be appropriate.
Exclusion Criteria:
NOTE: Resection of the gastric antrum, the appendix, descending colon, sigmoid colon and rectum are permitted if there is no overt evidence of malabsorption.
NOTE: Any ongoing potentially reversible toxicity from prior anti-cancer therapy that is > Grade 1 (except alopecia or Grade 2 neuropathy that has been stable for at least 4 weeks) or any toxicity from prior anti-cancer therapy that is progressing in severity will render the subject ineligible unless agreed to by the GSK Medical Monitor and the Investigator.
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| Name | Affiliation | Role |
|---|---|---|
| GSK Clinical Trials | GlaxoSmithKline | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| GSK Investigational Site | Scottsdale | Arizona | 85259 | United States | ||
| GSK Investigational Site |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 27140800 | Derived | Koch KM, Ferron-Brady G, Lemmon C, Cartee L, Hollyfield H, D'Amelio AM Jr, Piepszak A, Swaby RF, Curran D, Arya N. Bioequivalence study with lapatinib powder for oral suspension and the original tablet formulation in cancer patients. Clin Pharmacol Drug Dev. 2015 May-Jun;4(3):203-9. doi: 10.1002/cpdd.139. Epub 2014 Oct 27. |
| Label | URL |
|---|---|
| Results for study 112930 can be found on the GSK Clinical Study Register. | View source |
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| Response to questionnaire regarding taste, consistency, and subject acceptability of alternative formulations of lapatinib. | Day 1 and Day 7 in either Period1 or Period 2 |
| Tucson |
| Arizona |
| 85724 |
| United States |
| GSK Investigational Site | Washington D.C. | District of Columbia | 20007 | United States |
| GSK Investigational Site | Fort Myers | Florida | 33905 | United States |
| GSK Investigational Site | Atlanta | Georgia | 30341 | United States |
| GSK Investigational Site | Detroit | Michigan | 48202 | United States |
| GSK Investigational Site | Memphis | Tennessee | 38120 | United States |
| GSK Investigational Site | Nashville | Tennessee | 37203 | United States |
| GSK Investigational Site | Seoul | 120-752 | South Korea |
| ID | Term |
|---|---|
| D001943 | Breast Neoplasms |
| ID | Term |
|---|---|
| D009371 | Neoplasms by Site |
| D009369 | Neoplasms |
| D001941 | Breast Diseases |
| D012871 | Skin Diseases |
| D017437 | Skin and Connective Tissue Diseases |
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| ID | Term |
|---|---|
| D000077341 | Lapatinib |
| ID | Term |
|---|---|
| D011799 | Quinazolines |
| D006574 | Heterocyclic Compounds, 2-Ring |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
| D006571 | Heterocyclic Compounds |
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