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Amg 510,K RAS G12C inhibitor
- 1. DATTATREYA MUKHERJEE MEDICAL STUDENT AND INDEPENDENT INTERNATIONAL RESEARCHER JINAN UNIVERSITY SCHOOL OF MEDICINE INTERNATIONAL SCHOOL,JINAN UNIVERSITY P.R CHINA AMG 510- A KRAS INHIBITOR
- 2. RAS oncogene: Point Mutation H RAS : BLADDER CANCER N RAS: Hematopoietic tumours. K RAS: NON SMALL CELL LUNG CANCER(NSCLC),CA COLON, CA PANCREAS
- 3. K RAS: RAS FAMILY GTPase It is a gene that that acts as an ON/ OFF Gene KRAS, a member of Ras protein family, acts as a molecular on/off switch. When turned on , it recruits and activates proteins necessary for the proliferation of growth factor and ther receptors’ signal such as c-Raf and PI 3-kinase. Mutation in K RAS hampers the cell division and control on Cell Div lost mutation in point mutation NSCLC, CA Colon, CA Pancreas DEPENDS ON MAP KINASE PATHWAY Signalling mol, Receptor, Kinase core, Messengers
- 4. MECHANISM OF K RAS
- 5. PROBLEM TO PREPARE K RAS INHIBITOR For over 30 years, the protein KRAS is a major challenge in drug design. So far, there is no approved therapy for patients with KRAS mutations, which comprise around 25% of patients with lung cancer. KRAS G12C can cause 13% of adenocarcinoma of Lung and 1-3% Solid tumor, 3% Colorectal Cancer and Appendix Cancer. K RAS is tightly attached to the GTP. For this preparing Drug is tough. Smoking can cause K RAS mutation.
- 6. AMG 510: A ENTERIC ROUTE ANTINEOPLASTIC DRUG Amg 510 is first class Drug orks on KRAS G12C receptor. AMG 510 is inhibiting K RAS by converting GTP to GDP. The name K RAS G12C point mutation is named because Glycine is changing into Cysteine in 12th position. Cysteine has sulphur which is giving a great targeted therapy and tolerability. Indication: NSCLC, CA Colon
- 7. Mechanism of AMG 510
- 9. Conclusions AMG 510 is noble first in class irreversible inhibitor of KRASG12C. It acts on KRAS through targeted treatment and then it blocks the conversion of GTP to GDP. AMG 510 is well tolerable and less adverse effects. according to Marwan Fakih et al AMG 510 is well tolerated at the dose levels tested and has shown antitumor activity when administered as monotherapy to patient with advanced K RAS G12C mutant solid tumor.
- 10. THANK YOU !!!