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Treatment of advanced estrogen receptor positive breast cancer

An estrogen receptor, estrogen technology, applied in the field of breast cancer treatment, can solve problems such as harmful side effects

Pending Publication Date: 2021-02-09
ESTETRA S P R L
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, these powerful drugs have very harmful side effects

Method used

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  • Treatment of advanced estrogen receptor positive breast cancer
  • Treatment of advanced estrogen receptor positive breast cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] To assess the potential of the estetrol component to inhibit the growth of estrogen-deprived breast cancer cells, an in vitro study of long-term estrogen-deprived MCF7 breast cancer cells (LTED cells) was performed. LTED cells were deprived of estrogen, making them a suitable in vitro model to study drug effects in women on long-term use of inhibitors of estrogen activity.

[0078] LTED cells were plated in 6-well plates at a density of 30,000 cells per well. Cells were maintained in phenol red-free IMEM with 5% charcoal-treated FBS (DCC-FBS). On day 3, replace the medium with fresh phenol red-free IMEM with 5% DCC-FBS. Cells were then exposed to 6 different concentrations of estetrol ranging from 10 -12 M to 10 -5 M, or exposure to ethanol as vehicle control. For all experiments, the final vehicle concentration was 0.1% ethanol. Each treatment was performed in duplicate.

[0079] On day 5, the medium was changed and on day 7 the plates were analyzed for cytometry...

Embodiment 2

[0086] Plasma levels of estetrol were tested on days 7 and 14 in 9-10 female patients for each group taking (orally administered) 2, 10, 20 and 40 mg estetrol per day. For each dose group, the average trough level for all patients on these two days was calculated.

[0087] As shown in Table 2, the results showed good dose linearity. Furthermore, this study shows that these high dose levels of estetrol are well tolerated, whereas comparable doses of other estrogens can cause significant side effects, such as nausea, that negatively impact QOL.

[0088] Table 2 - Trough and C of estetrol as a function of oral dose administered max plasma level

[0089] Estimated oral dose per day (mg) Trough plasma level (pg / mL) C max Plasma level (pg / mL)

Embodiment 3

[0091] A multicentre study was conducted with recruitment lasting approximately 9 months.

[0092] Conduct an open-label, phase I / IIa trial, dose-escalation study with a 3+3 cohort design to determine the recommended dose of E4 for the treatment of patients with advanced breast cancer. Following completion of the Phase I portion of the study (ie, 4 weeks of treatment), patients received a further 8 weeks of treatment at their respective Phase I dose levels (Phase IIa portion of the study). Patients were treated for 12 weeks. Treatment continued after 12 weeks of treatment until patients withdrew from the study due to unacceptable adverse events (AEs) or disease progression. These patients were followed according to clinical practice including radiation oncology assessment.

[0093] target group : A total of at least 9 patients with ER+ locally advanced and / or metastatic breast cancer who had exhausted all treatment options were included in the study. Patients who have bee...

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Abstract

The invention relates to the treatment of advanced estrogen receptor positive breast cancer in a subject who has been treated with an estrogen activity suppressor selected from a selective estrogen receptor modulator (SERM), an aromatase inhibitor and an anti-estrogen, said treatment comprising administration of an estetrol componentafter the treatment with an estrogen activity suppressor has beendiscontinued, said estetrol component being selected from estetrol, prodrugs of estetrol and combinations thereof.

Description

[0001] field of invention [0002] The present invention relates to the field of breast cancer treatment. More specifically, the present invention relates to late estrogen receptor positive mammary glands in subjects who have been treated with inhibitors of estrogen activity selected from the group consisting of selective estrogen receptor modulators (SERMs), aromatase inhibitors and antiestrogens A treatment for cancer comprising administering an estetrol component selected from the group consisting of estetrol, prodrugs of estetrol, and combinations thereof within 12 weeks of cessation of estrogen-active inhibitor therapy. Background technique [0003] Breast cancer is one of the leading causes of cancer mortality among Western women and is expected to become the leading cause of cancer death among Eastern women in countries such as Japan in the near future. The American Cancer Society estimates that 1 in 9 women is at lifetime risk for the disease, which is fatal in about ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/565A61K45/06A61K9/00A61P35/00
CPCA61K31/565A61K45/06A61P5/30A61P35/00A61K9/0053
Inventor H·J·T·科尔林格本宁克C·费尔赫芬
Owner ESTETRA S P R L
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