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词条 Sacituzumab govitecan
释义

  1. Mechanism

  2. Development

  3. References

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| target = Trop-2
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| CAS_number = 1491917-83-9
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| C = 6496 | H = 9986 | N = 1702 | O = 2016 | S = 42
| molecular_weight = 154.4 g/mol
| UNII = M9BYU8XDQ6
| KEGG = D10985
| synonyms = IMMU-132, hRS7-SN-38
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Sacituzumab govitecan (IMMU-132 or hRS7-SN-38) is an investigational antibody-drug conjugate.[1] It is being developed by Immunomedics.

Mechanism

It is a conjugate of the humanized anti-Trop-2 monoclonal antibody linked with SN-38, the active metabolite of irinotecan.[2] Each antibody having on average 6.7 molecules of SN-38 attached.[3] SN-38 is too toxic to administer directly to patients, but linkage to an antibody allows the drug to specifically target cells containing Trop-2.

Development

Sacituzumab govitecan is an investigational drug that has not been FDA-approved for disease therapy. Immunomedics announced in 2013 that it had received an FDA fast track designation for the compound as a potential treatment for non-small cell lung cancer, small cell lung cancer, and metastatic triple-negative breast cancer. Orphan drug status was granted for small cell lung cancer and pancreatic cancer.[4]{{request quotation|date=December 2017}} In in February 2016, Immunomedics announced that sacituzumab govitecan had received an FDA breakthrough therapy designation (a classification designed to expedite the development and review of drugs that are intended, alone or in combination with one or more other drugs, to treat a serious or life-threatening disease or condition) for the treatment of patients with triple-negative breast cancer who have failed at least two other prior therapies for metastatic disease.[5]

References

1. ^FDA Fast Track for TNBC
2. ^[https://www.ncbi.nlm.nih.gov/pubmed/25915780 Sacituzumab Govitecan (IMMU-132), an Anti-Trop-2/SN-38 Antibody-Drug Conjugate: Characterization and Efficacy in Pancreatic, Gastric, and Other Cancers. 2015]
3. ^Novel Agents are Targeting Drivers of TNBC. 2016
4. ^http://adisinsight.springer.com/drugs/800037529
5. ^New Therapy Shows Early Promise, Continues to Progress in Triple-Negative Breast Cancer. Feb 2016
{{pharma-stub}}{{monoclonals for tumors}}

4 : Antibody-drug conjugates|Breakthrough therapy|Experimental cancer drugs|Orphan drugs

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