Antineoplastic Combinations Containing HKI-272 and Vinorelbine

a technology of hki-272 and vinorelbine, which is applied in the direction of heterocyclic compound active ingredients, drug compositions, biocides, etc., can solve the problems of cancer cells which are not recognized, the risk of toxicity increases, and the association of trastuzumab-based therapy with potential cardiac toxicity

Inactive Publication Date: 2009-12-17
WYETH LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the risk of toxicity increases in parallel with the number of previous anticancer treatments.
Trastuzumab-based therapy ...

Method used

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  • Antineoplastic Combinations Containing HKI-272 and Vinorelbine
  • Antineoplastic Combinations Containing HKI-272 and Vinorelbine
  • Antineoplastic Combinations Containing HKI-272 and Vinorelbine

Examples

Experimental program
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Effect test

example 1

Combination Regimen of HKI-272 and Vinorelbine in Lung Cancer Cell Proliferation Assays

[0108]A standard cell proliferation assay was utilized to independently analyze the response of lung cell lines NC1-H1666, NC1-H1650, and NC1-H1975 to various dilutions of HKI-272 and vinorelbine in combination. Briefly, fetal bovine serum (FBS) RPM1-1640 (Media) was added to each well of 96 well plates containing one of the cell lines. Each column of wells contained a different dilution of HKI-272 and solutions of vinorelbine were added to each well at a variety of dilutions with respect to the HKI-272 dilutions (the highest final concentration of HKI-272 was 1 μM for the H1650 and H1666 cell lines; the highest final concentration of HKI-272 was 9 μM for the H1975 cell line; and the highest final concentration of vinorelbine was 0.1 μM for all of the cell lines). Following incubation of the cell plates at 37° C., 5% CO2 for 72 hours, cell proliferation was assessed.

[0109]Cell proliferation was re...

example 2

Combination Regimen of HKI-272 and Vinorelbine in Treatment of Non-Metastatic Breast Cancers

[0110]Patients having diagnosed non-metastatic breast cancers are treated using a regimen of HKI-272 and vinorelbine. Patients are administered HKI-272 at either dose level 1 or 2. Dosing of HKI-272 begins at cycle 1, day 1 with daily oral administration of HKI-272 at the dosages in Table 3. HKI-272 is taken orally on the remaining days of the each cycle. On those days that HKI-272 and vinorelbine are administered on the same day, i.e., days 1 and 8 of the cycle, HKI-272 is administered prior to the vinorelbine infusion.

TABLE 3Dose LevelHKI-272 Dose (mg)Vinorelbine Dose (mg / m2)1160252240

[0111]Vinorelbine is administered on days 1 and 8 of each 21-day cycle, provided that the combination of HKI-272 and vinorelbine is well tolerated and there is no evidence of disease progression. Vinorelbine is administered intravenously using preferentially a central venous route, through a free-flowing IV li...

example 3

Combination Regimen of HKI-272 and Vonorelbine in Treatment of Metastatic Breast Cancers

[0114]Patients having diagnosed metastatic breast cancers are treated using a regimen of HKI-272 and vinorelbine.

[0115]Vinorelbine is administered on day 1 and day 8 of the cycle using the dosages described in Example 2, Table 3 or 5. The vinorelbine is administered over a 30-minute period using an in-line filter and an automatic dispensing pump. Optionally, antihistamine (diphenhydramine, 25 to 50 mg IV or the equivalent) is administered about 30 minutes prior to vinorelbine infusion.

[0116]Dosing of HKI-272 begins at cycle 1, day 2 with daily oral administration of HKI-272 at the dosages provided in Example 2, Table 3 or 4. HKI-272 is taken orally on the remaining days of the each cycle. On those days that HKI-272 and vinorelbine are administered on the same day, i.e., day 8 of the cycle, HKI-272 is administered prior to the vinorelbine infusion. If the patient has any serious side-effects durin...

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Abstract

A combination of HKI-272 compound and a vinorelbine compound in the treatment of a neoplasm is provided. Regimens, kits, and methods for treatment of neoplasm, including breast cancer including metastatic breast cancer, and lung cancer, using this combination, optionally in combination with other anti-neoplastic agents, or immune modulators are also described.

Description

BACKGROUND OF THE INVENTION[0001]Breast cancer is the most frequently diagnosed malignancy in women and one of the top two causes of cancer-related deaths in women worldwide. The incidence of breast cancer in the world is increasing, and it is estimated that the disease will affect 5 million women in the next decade. Treatments permit control of symptoms, prolongation of survival, and maintenance of quality of life. However, in about 40% to 50% of all patients treated with curative intent, incurable metastatic disease will develop. Since there is no cure for metastatic breast cancer, current therapeutic goals are palliative.[0002]In several cancer types, deregulation of growth factor signaling is observed, associated with a hyperactivation of the ErbB receptors. The ErbB receptor family includes ErbB-1 (also known as HER-1, epidermal growth factor receptor (EGFR)), ErbB-2 (a.k.a. neu or HER-2), HER-3 (a.k.a. ErbB-3), and HER-4 (a.k.a. ErbB-4). Overexpression of ErbB-1 is observed in...

Claims

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Application Information

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IPC IPC(8): A61K31/437A61P35/00
CPCA61K31/436A61K31/437A61K31/4745A61N5/10A61K31/475A61K31/4709A61K2300/00A61P15/00A61P35/00A61P35/04A61P43/00A61K31/164A61K9/20
Inventor ZACHARCHUK, CHARLES MICHAEL
Owner WYETH LLC
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