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Combination of a PI3 Kinase Inhibitor with Pacitaxel for Use in the Treatment or Prevention of a Cancer of the Head and Neck

a technology of pacitaxel and kinase inhibitor, which is applied in the field of combination of pi3 kinase inhibitor and pacitaxel for use in the treatment or prevention of head and neck cancer, can solve the problems of poor recurrence rate, poor progress, and ineffective palliative treatment of recurrent/metastatic hnscc, so as to reduce side effects, prolong the response, and delay the progression or inhibit the symptoms.

Inactive Publication Date: 2016-03-24
NOVARTIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent text describes a pharmaceutical combination of two drugs that can have different modes of action. When used together, the combination can produce better results than using either drug alone. The combination can have a synergistic effect, meaning that the drugs work together to produce a stronger effect than either drug alone. This combination can also have fewer side effects, be more durable, improve quality of life, and decrease the likelihood of the disease coming back. The text also explains how to determine if the combination is effective and how to measure the strength of the effect. The patent also mentions that animal models can be used to test the effectiveness of the combination. Overall, the patent describes a way to make drugs that work better together to treat disease.

Problems solved by technology

Palliative treatment of recurrent / metastatic HNSCC remains largely ineffective, and little progress has been made.
Although HNSCC can be considered a chemosensitive disease as shown by high response rates with aggressive induction therapies (e.g., combination of 5-FU, cisplatin and docetaxel, the results are poor at relapse.
Patients usually relapse locally and develop symptoms such as difficulties in swallowing, eating and speaking.

Method used

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  • Combination of a PI3 Kinase Inhibitor with Pacitaxel for Use in the Treatment or Prevention of a Cancer of the Head and Neck
  • Combination of a PI3 Kinase Inhibitor with Pacitaxel for Use in the Treatment or Prevention of a Cancer of the Head and Neck
  • Combination of a PI3 Kinase Inhibitor with Pacitaxel for Use in the Treatment or Prevention of a Cancer of the Head and Neck

Examples

Experimental program
Comparison scheme
Effect test

example 1

Sensitivity of Head and Neck Cancer Cell Lines to Compound A and to a Combination of Paclitaxel and Compound A

[0103]As shown in FIG. 1, two panels were independently tested for sensitivity to Compound A. The majority of the cell lines display an IC50 below 1 μM in line with clinically relevant concentrations (concentration delivered to patients treated at 100 mg daily is expected to be around 1 μM). (Red=KRAS mutant=UMSCC-74A. Yellow=PI3KCA mutant=CAL33).

[0104]As shown in FIG. 2, treatment of FaDu xenograft (Hypopharynx squamous cell carcinoma) with Compound A at 30 mg daily (equivalent to 100 mg daily in patients) shows inhibition of pAKT in tumor tissue confirming down-regulation of the PI3K pathway upon treatment. Treatment with Paclitaxel and Compound A in head and neck cancer cell lines displays combination effect with potential for synergy in some cases.

[0105]Cells were plated in 24-well plates at a density of 5×104 to 1×105 cells per well and grown in DMEM with 10% FBS and 1%...

example 2

Clinical Study

[0106]A clinical study using (a) a phosphatidylinositol 3-kinase inhibitor COMPOUND A or its hydrochloride salt, in combination with (b) paclitaxel for treatment of patients with recurrent or metastatic HNSCC cancer that has progressed after prior platinum based treatment regimen.

[0107]A multi-center, randomized, double-blind, placebo-controlled phase II trial of the combination comprising (a) COMPOUND A or its hydrochloride salt and (b) paclitaxel is conducted in patients with recurrent or metastatic HNSCC cancer that has progressed after prior platinum based treatment regimen. Patients with histologically / cytologically-confirmed HNSCC, recurrent or metastatic disease progressing after prior platinum-based first-line treatment will be randomized in a 1:1 ratio to 2 different clinical group arms to receive in a blinded manner one of two treatments: (a) COMPOUND A or its hydrochloride salt in combination with paclitaxel, or (b) placebo in combination with paclitaxel. Ap...

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Abstract

A pharmaceutical combination comprising (a) a phosphatidylinositol-3-kinase (PI3K) inhibitor compound of formula (I), as defined herein, or a pharmaceutically acceptable salt thereof and (b) paclitaxel or a pharmaceutically acceptable salt thereof for simultaneous, separate or sequential use, for the treatment of a cancer of the head and neck; a pharmaceutical composition comprising said combination; the use of said combination for the preparation of a medicament for the treatment of a cancer of the head and neck; a method of treating or preventing a cancer of the head and neck comprising administering a jointly therapeutically effective amount of such a combination to a subject in need thereof; and a commercial package thereof.

Description

FIELD OF THE INVENTION[0001]A pharmaceutical combination comprising (a) a phosphatidylinositol-3-kinase (PI3K) inhibitor compound of formula (I), as defined herein, or a pharmaceutically acceptable salt thereof and (b) paclitaxel or a pharmaceutically acceptable salt thereof for simultaneous, separate or sequential use, for the treatment of a cancer of the head and neck; a pharmaceutical composition comprising said combination; the use of said combination for the preparation of a medicament for the treatment of a cancer of the head and neck; a method of treating or preventing a cancer of the head and neck comprising administering a jointly therapeutically effective amount of such a combination to a subject in need thereof; and a commercial package thereof.BACKGROUND OF THE INVENTION[0002]Cancer of the head and neck includes all cancers arising from the upper aerodigestive tract. Squamous cell carcinomas originating from mucosal surfaces represent more than 90% of cases. The incidenc...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/5377A61K31/337
CPCA61K31/337A61K31/5377A61K31/5395A61P1/02A61P35/00A61P43/00A61K2300/00A61K31/506
Inventor HIRAWAT, SAMITMASSACESI, CRISTIANDI, TOMASO, EMMANUELLE
Owner NOVARTIS AG
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