Antibody-conjugates for targeting of tumours expressing trop-2
What is Al technical title?
Al technical title is built by PatSnap Al team. It summarizes the technical point description of the patent document.
A technology of conjugates and antibodies, which can be used in anti-tumor drugs, drug combinations, medical preparations of inactive ingredients, etc., can solve the problems of instability, high cost, time-consuming, etc., and achieve the effect of improving the therapeutic index
Pending Publication Date: 2021-08-13
SYNAFFIX
View PDF22 Cites 0 Cited by
Summary
Abstract
Description
Claims
Application Information
AI Technical Summary
This helps you quickly interpret patents by identifying the three key elements:
Problems solved by technology
Method used
Benefits of technology
Problems solved by technology
However, the latter approach has the disadvantage of having to redesign the native sequence of the antibody, which is not only time-consuming and expensive, but can also lead to instability problems
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
Click on the blue label to locate the original text in one second.
Reading with bidirectional positioning of images and text.
Smart Image
Examples
Experimental program
Comparison scheme
Effect test
Embodiment Construction
[0028] In a first aspect, the invention relates to antibody conjugates. In connection with this, in a second aspect, the present invention relates to a method of preparing an antibody conjugate of the invention. In a third aspect, the invention relates to methods for targeting cells expressing Trop-2. Related thereto is a first medical use of the antibody conjugates of the invention, and a second medical use for the treatment of cancer. In a last aspect, the present invention relates to the use of conjugation means for increasing the therapeutic index of antibody conjugates in the treatment of Trop-2 expressing tumors.
[0029] definition
[0030] As used in this specification and claims, the verb "to comprise" and its conjugations are used in its non-limiting sense to mean that items following the word are included, but items not specifically mentioned are not excluded.
[0031] Also, reference to an element with the indefinite article "a" or "an" does not preclude the p...
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
Login to view more
Abstract
The present invention concerns antibody-conjugate having general structure (2): AB-[(L 6 )-{Z-(L1) n -(L2 ) o -(L3 ) p-(L4 ) q-D} xx ] yy (2) wherein AB is an antibody capable of targeting Trop-2-expressing tumours and D is selected from the group consisting of taxanes, anthracyclines, camptothecins, epothilones, mytomycins, combretastatins, vinca alkaloids, maytansinoids, enediynes such as calicheamicins, duocarmycins, tubulysins, amatoxins, bleomycins, dolastatins and auristatins, pyrrolobenzodiazepine dimers, indolinobenzodiazepine dimers, radioisotopes, therapeutic proteins and peptides (or fragments thereof), kinase inhibitors, MEK inhibitors, KSP inhibitors, and analogues or prodrugs thereof. These antibody-conjugates exhibit an improved therapeutic index. The invention further concerns a process for preparing the antibody-conjugate according to the invention, a method for targeting Trop-2-expressing cells, medical uses of the antibody-conjugates according to the invention.
Description
technical field [0001] The present invention is in the field of bioconjugation. More specifically, the present invention relates to antibody-drug conjugates for the targeted therapy of patients with cancer, particularly Trop-2 expressing tumors. Background technique [0002] Proteins that play a role in the growth, differentiation, invasion and / or metastasis of breast cancer can affect the biological course of the tumor and thus provide important prognostic information. One such candidate is Trop-2 (GA733-1, EGP-1), a 45 kDa monomeric transmembrane glycoprotein belonging to the TACSTD gene family, specifically TACSTD2, which is expressed in human epithelial cells at various stages of differentiation. expressed in cells. Overexpression of Trop-2 has been shown to be necessary and sufficient to stimulate tumor growth and is associated with poor overall prognosis. Trop-2 expression is associated with poor prognosis in several human cancers, including oral, pancreatic, gastri...
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
Application Date:The date an application was filed.
Publication Date:The date a patent or application was officially published.
First Publication Date:The earliest publication date of a patent with the same application number.
Issue Date:Publication date of the patent grant document.
PCT Entry Date:The Entry date of PCT National Phase.
Estimated Expiry Date:The statutory expiry date of a patent right according to the Patent Law, and it is the longest term of protection that the patent right can achieve without the termination of the patent right due to other reasons(Term extension factor has been taken into account ).
Invalid Date:Actual expiry date is based on effective date or publication date of legal transaction data of invalid patent.
Login to view more 
Login to view more