Medicinal Chemistry II (15) Plant Products = Vincristine, Vinblastine, Etoposide and Miscellaneous
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1. Vincristine and Vinblastine:
a. Chemistry: Vincristine and vinblastine are both vinca alkaloids derived from the periwinkle plant (Catharanthus roseus). They share a similar core structure and are structurally complex molecules.
b. Mechanism of Action: These drugs bind to tubulin, a protein that makes up microtubules, essential for cell division. By binding to tubulin, they disrupt the formation of microtubules, preventing proper mitotic spindle assembly, and leading to cell cycle arrest.
c. Clinical Use: Vincristine and vinblastine are used in chemotherapy regimens to treat a variety of cancers, including leukemias, lymphomas, and solid tumors.
2. Etoposide:
a. Chemistry: Etoposide is a semi-synthetic derivative of podophyllotoxin, a naturally occurring compound. Its chemical structure includes a planar, aromatic ring system.
b. Mechanism of Action: Etoposide is a topoisomerase II inhibitor. It forms a ternary complex with topoisomerase II and DNA, preventing DNA re-ligation after the enzyme makes a double-strand break. This leads to accumulation of DNA breaks and cell death.
c. Clinical Use: Etoposide is used in the treatment of various cancers, including lung cancer, testicular cancer, and certain types of leukemia.
Miscellaneous Agents:
3. Imatinib:
a. Chemistry: Imatinib is a small molecule tyrosine kinase inhibitor (TKI) designed to specifically target the BCR-ABL fusion protein, an abnormal kinase found in chronic myeloid leukemia (CML).
b. Mechanism of Action: Imatinib competes with ATP to bind the BCR-ABL kinase domain, inhibiting its activity and blocking the aberrant signaling that drives cancer growth.
c. Clinical Use: Imatinib is used to treat CML and certain forms of gastrointestinal stromal tumors (GISTs) that express mutant KIT or PDGFRA.
4. Bortezomib:
a. Chemistry: Bortezomib is a proteasome inhibitor, a small peptide-like molecule.
b. Mechanism of Action: Bortezomib reversibly binds to the 26S proteasome, preventing the degradation of targeted proteins. This leads to the accumulation of regulatory proteins, cell cycle arrest, and apoptosis.
c. Clinical Use: Bortezomib is used to treat multiple myeloma and mantle cell lymphoma.
5. Trastuzumab:
a. Chemistry: Trastuzumab is a monoclonal antibody produced using recombinant DNA technology.
b. Mechanism of Action: Trastuzumab targets the HER2/neu receptor, inhibiting its signaling pathways and promoting immune-mediated destruction of HER2-positive cancer cells.
c. Clinical Use: Trastuzumab is used to treat HER2-positive breast cancer.
6. Pemetrexed:
a. Chemistry: Pemetrexed is a folate antimetabolite that structurally resembles folic acid.
b. Mechanism of Action: Pemetrexed inhibits multiple enzymes involved in folate-dependent pathways, disrupting DNA and RNA synthesis.
c. Clinical Use: Pemetrexed is used to treat lung cancer and mesothelioma.
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1. Vincristine and Vinblastine:
a. Chemistry: Vincristine and vinblastine are both vinca alkaloids derived from the periwinkle plant (Catharanthus roseus). They share a similar core structure and are structurally complex molecules.
b. Mechanism of Action: These drugs bind to tubulin, a protein that makes up microtubules, essential for cell division. By binding to tubulin, they disrupt the formation of microtubules, preventing proper mitotic spindle assembly, and leading to cell cycle arrest.
c. Clinical Use: Vincristine and vinblastine are used in chemotherapy regimens to treat a variety of cancers, including leukemias, lymphomas, and solid tumors.
2. Etoposide:
a. Chemistry: Etoposide is a semi-synthetic derivative of podophyllotoxin, a naturally occurring compound. Its chemical structure includes a planar, aromatic ring system.
b. Mechanism of Action: Etoposide is a topoisomerase II inhibitor. It forms a ternary complex with topoisomerase II and DNA, preventing DNA re-ligation after the enzyme makes a double-strand break. This leads to accumulation of DNA breaks and cell death.
c. Clinical Use: Etoposide is used in the treatment of various cancers, including lung cancer, testicular cancer, and certain types of leukemia.
Miscellaneous Agents:
3. Imatinib:
a. Chemistry: Imatinib is a small molecule tyrosine kinase inhibitor (TKI) designed to specifically target the BCR-ABL fusion protein, an abnormal kinase found in chronic myeloid leukemia (CML).
b. Mechanism of Action: Imatinib competes with ATP to bind the BCR-ABL kinase domain, inhibiting its activity and blocking the aberrant signaling that drives cancer growth.
c. Clinical Use: Imatinib is used to treat CML and certain forms of gastrointestinal stromal tumors (GISTs) that express mutant KIT or PDGFRA.
4. Bortezomib:
a. Chemistry: Bortezomib is a proteasome inhibitor, a small peptide-like molecule.
b. Mechanism of Action: Bortezomib reversibly binds to the 26S proteasome, preventing the degradation of targeted proteins. This leads to the accumulation of regulatory proteins, cell cycle arrest, and apoptosis.
c. Clinical Use: Bortezomib is used to treat multiple myeloma and mantle cell lymphoma.
5. Trastuzumab:
a. Chemistry: Trastuzumab is a monoclonal antibody produced using recombinant DNA technology.
b. Mechanism of Action: Trastuzumab targets the HER2/neu receptor, inhibiting its signaling pathways and promoting immune-mediated destruction of HER2-positive cancer cells.
c. Clinical Use: Trastuzumab is used to treat HER2-positive breast cancer.
6. Pemetrexed:
a. Chemistry: Pemetrexed is a folate antimetabolite that structurally resembles folic acid.
b. Mechanism of Action: Pemetrexed inhibits multiple enzymes involved in folate-dependent pathways, disrupting DNA and RNA synthesis.
c. Clinical Use: Pemetrexed is used to treat lung cancer and mesothelioma.
Get in touch with the solution by just clicking the following links-
Facebook Group- Facebook: solutionpharamcy
Mobile App - https://play.google.com/store/apps/de...
New Channel (Pharmacy Dictionary) @pharmacydictionary
E-Mail for official and other work - [email protected]
#solutionpharmacy #Pharmacologyclass #Pharmacognosyvideos #GPAT
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