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Emtansine
Mertansine, also called DM1 (and #Emtansine, in some of its forms emtansine), is a thiol-containing maytansinoid that for therapeutic purposes is attached to a monoclonal antibody through reaction of the thiol group with a linker structure to create an antibody-drug conjugate (ADC). ADCs with this design include trastuzumab emtansine, lorvotuzumab mertansine, and cantuzumab mertansine. Some are still experimental; others are in regular clinical use. Mechanism of action Mertansine is a tubulin inhibitor, meaning that it inhibits the assembly of microtubules by binding to tubulin (at the rhizoxin binding site).National Cancer InstituteDefinition of Maytansine/ref> The monoclonal antibody binds specifically to a structure (usually a protein) occurring in a tumour, thus directing mertansine into this tumour. This concept is called targeted therapy. Uses and chemistry The following (experimental) drugs are antibody-drug conjugates (ADC) combining monoclonal antibodies with mertansin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Trastuzumab Emtansine
Trastuzumab emtansine, sold under the brand name Kadcyla, is an antibody-drug conjugate consisting of the humanized monoclonal antibody trastuzumab (Herceptin) covalently linked to the cytotoxic agent DM1. Trastuzumab alone stops growth of cancer cells by binding to the HER2 receptor, whereas trastuzumab emtansine undergoes receptor-mediated internalization into cells, is catabolized in lysosomes where DM1-containing catabolites are released and subsequently bind tubulin to cause mitotic arrest and cell death. Trastuzumab binding to HER2 prevents homodimerization or heterodimerization (HER2/HER3) of the receptor, ultimately inhibiting the activation of MAPK and PI3K/AKT cellular signalling pathways. Because the monoclonal antibody targets HER2, and HER2 is only over-expressed in cancer cells, the conjugate delivers the cytotoxic agent DM1 specifically to tumor cells. The conjugate is abbreviated T-DM1. In the EMILIA clinical trial of women with advanced HER2 positive breast ca ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Trastuzumab Emtansine
Trastuzumab emtansine, sold under the brand name Kadcyla, is an antibody-drug conjugate consisting of the humanized monoclonal antibody trastuzumab (Herceptin) covalently linked to the cytotoxic agent DM1. Trastuzumab alone stops growth of cancer cells by binding to the HER2 receptor, whereas trastuzumab emtansine undergoes receptor-mediated internalization into cells, is catabolized in lysosomes where DM1-containing catabolites are released and subsequently bind tubulin to cause mitotic arrest and cell death. Trastuzumab binding to HER2 prevents homodimerization or heterodimerization (HER2/HER3) of the receptor, ultimately inhibiting the activation of MAPK and PI3K/AKT cellular signalling pathways. Because the monoclonal antibody targets HER2, and HER2 is only over-expressed in cancer cells, the conjugate delivers the cytotoxic agent DM1 specifically to tumor cells. The conjugate is abbreviated T-DM1. In the EMILIA clinical trial of women with advanced HER2 positive breast ca ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Emtansine
Mertansine, also called DM1 (and #Emtansine, in some of its forms emtansine), is a thiol-containing maytansinoid that for therapeutic purposes is attached to a monoclonal antibody through reaction of the thiol group with a linker structure to create an antibody-drug conjugate (ADC). ADCs with this design include trastuzumab emtansine, lorvotuzumab mertansine, and cantuzumab mertansine. Some are still experimental; others are in regular clinical use. Mechanism of action Mertansine is a tubulin inhibitor, meaning that it inhibits the assembly of microtubules by binding to tubulin (at the rhizoxin binding site).National Cancer InstituteDefinition of Maytansine/ref> The monoclonal antibody binds specifically to a structure (usually a protein) occurring in a tumour, thus directing mertansine into this tumour. This concept is called targeted therapy. Uses and chemistry The following (experimental) drugs are antibody-drug conjugates (ADC) combining monoclonal antibodies with mertansin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mertansine Mab Structure Coloured
Mertansine, also called DM1 (and in some of its forms emtansine), is a thiol-containing maytansinoid that for therapeutic purposes is attached to a monoclonal antibody through reaction of the thiol group with a linker structure to create an antibody-drug conjugate (ADC). ADCs with this design include trastuzumab emtansine, lorvotuzumab mertansine, and cantuzumab mertansine. Some are still experimental; others are in regular clinical use. Mechanism of action Mertansine is a tubulin inhibitor, meaning that it inhibits the assembly of microtubules by binding to tubulin (at the rhizoxin binding site).National Cancer InstituteDefinition of Maytansine/ref> The monoclonal antibody binds specifically to a structure (usually a protein) occurring in a tumour, thus directing mertansine into this tumour. This concept is called targeted therapy. Uses and chemistry The following (experimental) drugs are antibody-drug conjugates (ADC) combining monoclonal antibodies with mertansine as the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Emtansine Mab Structure Coloured
Mertansine, also called DM1 (and in some of its forms emtansine), is a thiol-containing maytansinoid that for therapeutic purposes is attached to a monoclonal antibody through reaction of the thiol group with a linker structure to create an antibody-drug conjugate (ADC). ADCs with this design include trastuzumab emtansine, lorvotuzumab mertansine, and cantuzumab mertansine. Some are still experimental; others are in regular clinical use. Mechanism of action Mertansine is a tubulin inhibitor, meaning that it inhibits the assembly of microtubules by binding to tubulin (at the rhizoxin binding site).National Cancer InstituteDefinition of Maytansine/ref> The monoclonal antibody binds specifically to a structure (usually a protein) occurring in a tumour, thus directing mertansine into this tumour. This concept is called targeted therapy. Uses and chemistry The following (experimental) drugs are antibody-drug conjugates (ADC) combining monoclonal antibodies with mertansine as the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antibody-drug Conjugate
Antibody-drug conjugates or ADCs are a class of biopharmaceutical drugs designed as a targeted therapy for treating cancer. Unlike chemotherapy, ADCs are intended to target and kill tumor cells while sparing healthy cells. As of 2019, some 56 pharmaceutical companies were developing ADCs. ADCs are complex molecules composed of an antibody linked to a biologically active cytotoxic (anticancer) payload or drug. Antibody-drug conjugates are an example of bioconjugates and immunoconjugates. ADCs combine the targeting properties of Monoclonal antibody, monoclonal antibodies with the cancer-killing capabilities of cytotoxic drugs, designed to discriminate between healthy and diseased tissue. Mechanism of action An anticancer drug is coupled to an antibody that targets a specific tumor antigen (or protein) that, ideally, is only found in or on tumor cells. Antibodies attach themselves to the antigens on the surface of cancerous cells. The biochemical reaction that occurs upon attaching ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Maytansinoid
Maitansine (INN), or maytansine (USAN), is a cytotoxic agent. It inhibits the assembly of microtubules by binding to tubulin at the rhizoxin binding site. It is a macrolide of the ansamycin type and can be isolated from plants of the genus ''Maytenus''. Maytansinoids Derivatives of maitansine are known as maytansinoids. Some are being investigated as the cytotoxic component of antibody-drug conjugates for cancer treatment, and the antibody-drug conjugate trastuzumab emtansine is an approved drug for the treatment of certain kinds of breast cancer in the EU and in the US. Examples of maytansinoids are: * Ansamitocin *Mertansine / emtansine (DM1) * Ravtansine / soravtansine (DM4) See also * ImmunoGen An immunogen is any substance that generates B-cell (humoral/antibody) and/or T-cell (cellular) adaptive immune responses upon exposure to a host organism. Immunogens that generate antibodies are called antigens ("antibody-generating"). Immunogen ..., developer of maytansinoid base ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lorvotuzumab Mertansine
Lorvotuzumab mertansine (IMGN901) is an antibody-drug conjugate. It comprises the CD56-binding antibody, lorvotuzumab (huN901), with a maytansinoid cell-killing agent, DM1, attached using a disulfide linker, SPP. (When DM1 is attached to an antibody with the SPP linker, it is mertansine; when it is attached with the thioether linker, SMCC, it is emtansine.) Lorvotuzumab mertansine is an experimental agent created for the treatment of CD56 positive cancers (e.g. small-cell lung cancer, ovarian cancer). It has been granted Orphan drug status for Merkel cell carcinoma. It has reported encouraging Phase II results for small-cell lung cancer Small-cell carcinoma is a type of highly malignant cancer that most commonly arises within the lung, although it can occasionally arise in other body sites, such as the cervix, prostate, and gastrointestinal tract. Compared to non-small cell c .... References Antibody-drug conjugates Experimental cancer drugs Monoclonal antibodie ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
HER2/neu
Receptor tyrosine-protein kinase erbB-2 is a protein that in humans is encoded by the ''ERBB2'' gene. ERBB is abbreviated from erythroblastic oncogene B, a gene originally isolated from the avian genome. The human protein is also frequently referred to as ''HER2'' (human epidermal growth factor receptor 2) or CD340 (cluster of differentiation 340). HER2 is a member of the human epidermal growth factor receptor (HER/EGFR/ERBB) family. But contrary to other member of the ERBB family, HER2 does not directly bind ligand. HER2 activation results from heterodimerization with another ERBB member or by homodimerization when HER2 concentration are high, for instance in cancer. Amplification or over-expression of this oncogene has been shown to play an important role in the development and progression of certain aggressive types of breast cancer. In recent years the protein has become an important biomarker and target of therapy for approximately 30% of breast cancer patients. Name ''H ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lorvotuzumab Mertansine
Lorvotuzumab mertansine (IMGN901) is an antibody-drug conjugate. It comprises the CD56-binding antibody, lorvotuzumab (huN901), with a maytansinoid cell-killing agent, DM1, attached using a disulfide linker, SPP. (When DM1 is attached to an antibody with the SPP linker, it is mertansine; when it is attached with the thioether linker, SMCC, it is emtansine.) Lorvotuzumab mertansine is an experimental agent created for the treatment of CD56 positive cancers (e.g. small-cell lung cancer, ovarian cancer). It has been granted Orphan drug status for Merkel cell carcinoma. It has reported encouraging Phase II results for small-cell lung cancer Small-cell carcinoma is a type of highly malignant cancer that most commonly arises within the lung, although it can occasionally arise in other body sites, such as the cervix, prostate, and gastrointestinal tract. Compared to non-small cell c .... References Antibody-drug conjugates Experimental cancer drugs Monoclonal antibodie ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ImmunoGen
An immunogen is any substance that generates B-cell (humoral/antibody) and/or T-cell (cellular) adaptive immune responses upon exposure to a host organism. Immunogens that generate antibodies are called antigens ("antibody-generating"). Immunogens that generate antibodies are directly bound by host antibodies and lead to the selective expansion of antigen-specific B-cells. Immunogens that generate T-cells are indirectly bound by host T-cells after processing and presentation by host antigen-presenting cells. An immunogen can be defined as a complete antigen which is composed of the macromolecular carrier and epitopes (determinants) that can induce immune response. An explicit example is a hapten. Haptens are low-molecular-weight compounds that may be bound by antibodies, but cannot elicit an immune response. Consequently, the haptens themselves are nonimmunogenic and they cannot evoke an immune response until they bind with a larger carrier immunogenic molecule. The hapten-carrie ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Imide
In organic chemistry, an imide is a functional group consisting of two acyl groups bound to nitrogen. The compounds are structurally related to acid anhydrides, although imides are more resistant to hydrolysis. In terms of commercial applications, imides are best known as components of high-strength polymers, called polyimides. Inorganic imides are also known as solid state or gaseous compounds, and the imido group (=NH) can also act as a ligand. Nomenclature Most imides are cyclic compounds derived from dicarboxylic acids, and their names reflect the parent acid. Examples are succinimide, derived from succinic acid, and phthalimide, derived from phthalic acid. For imides derived from amines (as opposed to ammonia), the ''N''-substituent is indicated by a prefix. For example, N-ethylsuccinimide is derived from succinic acid and ethylamine. Isoimides are isomeric with normal imides and have the formula RC(O)OC(NR′)R″. They are often intermediates that convert to the more symmet ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
