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Mertansine
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] |
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] |
Cantuzumab Mertansine
Cantuzumab mertansine (SB-408075; huC242-DM1) is an antibody-drug conjugate investigated to treat colorectal cancer and other types of cancer. It is a humanized monoclonal antibody, cantuzumab (huC242) linked to a cytotoxic agent, mertansine (DM1). It was developed by ImmunoGen. Mechanism After the huC242 mab binds to the external domain of CanAg, the cantuzumab mertansine-CanAg complex is internalized, and the DM1 molecules are released intracellularly by cleavage of the DM1-huC242 disulfide bond In biochemistry, a disulfide (or disulphide in British English) refers to a functional group with the structure . The linkage is also called an SS-bond or sometimes a disulfide bridge and is usually derived by the coupling of two thiol groups. In ...s. Clinical trials Three phase I clinical studies had reported results by 2003. By 2005, clinical development had been suspended. See also * Cantuzumab ravtansine References Antibody-drug conjugates Monoclonal antibodies for ... [...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] |
Cantuzumab Mertansine
Cantuzumab mertansine (SB-408075; huC242-DM1) is an antibody-drug conjugate investigated to treat colorectal cancer and other types of cancer. It is a humanized monoclonal antibody, cantuzumab (huC242) linked to a cytotoxic agent, mertansine (DM1). It was developed by ImmunoGen. Mechanism After the huC242 mab binds to the external domain of CanAg, the cantuzumab mertansine-CanAg complex is internalized, and the DM1 molecules are released intracellularly by cleavage of the DM1-huC242 disulfide bond In biochemistry, a disulfide (or disulphide in British English) refers to a functional group with the structure . The linkage is also called an SS-bond or sometimes a disulfide bridge and is usually derived by the coupling of two thiol groups. In ...s. Clinical trials Three phase I clinical studies had reported results by 2003. By 2005, clinical development had been suspended. See also * Cantuzumab ravtansine References Antibody-drug conjugates Monoclonal antibodies for ... [...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] |
Bivatuzumab Mertansine
Bivatuzumab mertansine is a combination of bivatuzumab, a humanized monoclonal antibody, and mertansine, a cytotoxic agent. It is designed for the treatment of squamous cell carcinoma Squamous-cell carcinomas (SCCs), also known as epidermoid carcinomas, comprise a number of different types of cancer that begin in squamous cells. These cells form on the surface of the skin, on the lining of hollow organs in the body, and on the .... References Monoclonal antibodies for tumors Experimental cancer drugs Antibody-drug conjugates {{antineoplastic-drug-stub ... [...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] |
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] |
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] |
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] |
Multiple Myeloma
Multiple myeloma (MM), also known as plasma cell myeloma and simply myeloma, is a cancer of plasma cells, a type of white blood cell that normally produces antibodies. Often, no symptoms are noticed initially. As it progresses, bone pain, anemia, kidney dysfunction, and infections may occur. Complications may include amyloidosis. The cause of multiple myeloma is unknown. Risk factors include obesity, radiation exposure, family history, and certain chemicals. There is an increased risk of multiple myeloma in certain occupations. This is due to the occupational exposure to aromatic hydrocarbon solvents having a role in causation of multiple myeloma. Multiple myeloma may develop from monoclonal gammopathy of undetermined significance that progresses to smoldering myeloma. The abnormal plasma cells produce abnormal antibodies, which can cause kidney problems and overly thick blood. The plasma cells can also form a mass in the bone marrow or soft tissue. When one tumor i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
