Pharmaceutical composition containing crenolanib and application of pharmaceutical composition

A technology of clalanib and its use, which is applied in the field of pharmaceutical compositions containing clalanib and its use, and can solve problems such as dose escalation and treatment end

Inactive Publication Date: 2020-02-28
AROG PHARMA
View PDF6 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although toxicity can only be approximated and qualitatively assessed in such a small group, unanticipated toxicities led to discontinuation of planned dose escalation and end of treatment

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Pharmaceutical composition containing crenolanib and application of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0057] Preparation of Compounds of the Invention. General synthetic methods for preparing compounds of formula I are provided in, for example, U.S. Patent No. 5,990,146 (issued November 23, 1999) (Warner-Lambert Co.) and PCT Published Application No. WO 99 / 16755 (published April 8, 1999) (Merck & Co.), WO 01 / 40217 (published July 7, 2001) (Pfizer, Inc.), U.S. Patent Application Publication No. US 2005 / 0124599 (Pfizer, Inc.) and US Patent No. 7,183,414 (Pfizer, Inc.), in relevant part, is incorporated herein by reference.

[0058] Pharmaceutically acceptable salts such as hydrochloride, phosphate and lactate are prepared in a similar manner to the besylate salts and are well known to those of ordinary skill in the art. The following representative compounds of the invention are for illustrative purposes only and are by no means meant to limit the invention, including clalanid besylate, clalanide phosphate, clalanide lactate, clalanide hydrochloride, lemon Clairaninate, Clella...

Embodiment 1

[0060] Efficacy of combination therapy with clalanib besylate in patients with gastroesophageal junction (GEJ) adenocarcinoma with liver metastases: partial response according to RECIST 1.1 criteria.

[0061] A 53-year-old male was initially diagnosed with esophageal cancer in September 2017. Patients received palliative FOLFOX chemotherapy: a combination of a fluoropyrimidine (fluorouracil or 5-FU), a platinum compound (oxaliplatin) and leucovorin. Palliative chemotherapy started in late September 2017 and continued until January 2018. The patient was then given oral capecitabine for 5 months until June 2018 when the patient's cancer progressed. CT scans showed that the patient had progressive disease and the cancer had metastasized to the liver, upper stomach and lymph nodes.

[0062] For disease progression on first-line therapy, this patient was offered oral clalanib besylate (PDGFRβ inhibitor) with paclitaxel and ramucirumab in a second-line clinical trial of advanced es...

Embodiment 2

[0064] Efficacy of combined therapy of clalanib besylate in patients with stage IIIB gastric adenocarcinoma with metastasis to lymph nodes: Partial response was assessed according to RECIST 1.1 criteria.

[0065] A 68-year-old woman was diagnosed in September 2015 with stage IIIB metastatic cancer in the stomach and lymph nodes. She underwent partial gastrectomy and started adjuvant FOLFOX chemotherapy in October 2015. She remained on the FOLFOX regimen for 12 cycles until April 2016. Despite adjuvant chemotherapy, a CAT scan in October 2016 showed increased metastatic disease in the lymph nodes, which prompted palliative chemotherapy with fluorouracil. The patient continued to progress and was found to have metastatic disease to the gastrointestinal ligaments, lungs, and lymph nodes in October 2017.

[0066] Oral clalanib besylate (PDGFRβ inhibitor) was given to patients in combination with paclitaxel and ramucirumab in a second-line clinical trial (NCT03193918) of advanced...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention relates to a pharmaceutical composition containing crenolanib and application of the pharmaceutical composition. The present invention relates to the use of a combination comprising crenolanib or a salt thereof and a VEGF / VEGFR inhibitor of non-axitinib for the preparation of a medicament for the treatment of proliferative diseases, wherein the crenolanib and the VEGF / VEGFR inhibitorof non-axitinib are provided for a subject in at least one of a sequential or simultaneous manner for treating proliferative diseases, and the subject is a human subject.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to U.S. Provisional Application No. 62 / 779,128 (filed December 20, 2018) and U.S. Provisional Application No. 62 / 861,424 (filed June 20, 2019), the entire contents of which are incorporated by reference here. technical field [0003] The present invention relates to crenolanib or its salt and a non-axitinib VEGF / VEGFR inhibitor for the treatment of proliferative diseases, and a treatment method for warm-blooded animals, especially humans, wherein the The treatment method described above is to administer a therapeutically effective dose of clalanib and a non-axitinib VEGF / VEGFR inhibitor to a subject suffering from the disease or disorder. Background technique [0004] Without limiting the scope of the invention, its background can be described in relation to the treatment of cancer and the use of novel combination therapies including clalanib. [0005] Regarding this combination thera...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4709A61K45/06A61P35/00
CPCA61K31/4709A61K45/06A61P35/00A61K31/337C07K16/2863C07K2317/21A61K39/3955A61K2300/00
Inventor 维奈·K·柴恩
Owner AROG PHARMA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products