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Anticancer agents - 2, Drugs acting on G2M Phase, mitoxantrone, Bleomycin,…
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mitoxantrone
Used in advanced hormone resistance prostate cancer, AML, and breast cancer
and treatment of late stage secondary progressive multiple sclerosis.
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Bleomycin
Uses:
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• Part of the ABVD regimen (doxorubicin [Adriamycin], bleomycin, vinblastine, and dacarbazine)
Bleomycin is a CCS glycopeptide drug that acts in G2 phase by causing DNA strand breakage and free radical formation.
mitomycin
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It may be used as an intravesical therapy to treat superficial bladder cancers and anal carcinoma with radiation therapy.
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erlotinib
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the side effects of erlotinib:
Acneiform skin rash, diarrhea, anorexia and fatigue.
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relation between bleomycin and type 1,2 pneumocytes
It causes necrosis of type 1 pneumocytes
that results in compensatory hyperplasia of type 2 pneumocytes.
Bleomycin metabolism
Bleomycin is metabolized by bleomycin hydrolase
whose concentration is less in skin and lungs.
Thus the major organs involved in toxicity.
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geftinib and erlotinib
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Erlotinib is specially effective in cases affecting women,
non smokers, persons of asian ethnicity
as well as cases involving adenocarcinoma and bronchoalveolar carcinoma histology.
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sorafenib and sunitinib
Small molecule that inhibits multiple tyrosine kinases.
Both can be used for renal cell cancer.
In addition sorafenib indicated for hepatocellular carcinoma and sunitinib for GIST.
These can cause hypertension as adverse effect.
lapatinib
Indicated for breast carcinoma.
It inhibits tyrosine kinase associated with EGFR and her2/neu receptors.
pazopanib
It is a multitargeted tyrosine kinase inhibitor against VEGF receptors, PDGF receptor and C-kit.
Approved for treatment of advanced renal cell carcinoma.
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use of ruxolitinib
Myelofibrosis
Targets JAK 1, 2.
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proteasome inhibitors
Bortezomib, carfilzomib and ixazomib act by inhibiting proteasome resulting in downregulation of NFkB involved in cell survival.
Have been approved for resistant cases of multiple myeloma.
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mTOR inhibitors
This group includes everolimus and temsirolimus a prodrug that is converted into sirolimus.
Act as specific inhibitors of mTOR.
Temsirolimus approved for advanced renal cell carcinoma
whereas everolimus used for breast, brain, pancreas and renal cell carcinoma.
These are associated with interstitial lung disease.
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CDK inhibitors
Palbociclib is an orally effective cyclin dependent kinase CDK 4 and 6 inhibitor.
Approved in combination with letrozole for post menopausal women with ER + with HER 2 negative breast cancer.
PI3 kinase inhibitors
Idelalisib is a small molecule inhibitor of PI3 kinase delta.
Approved for oral treatment of relapsed CLL, follicular B cell NHL and SLL.
apoptosis inducers
Ingenol mebutate is an inducer of apoptosis
specifically indicated for
topical treatment of actinic keratosis of face, scalp, trunk and extremities
Omacetaxine
Omacetaxine is a protein synthesis inhibitor approved for chronic phase of CML.
It binds to A site and prevents elongation step in protein synthesis.
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bevacizumab
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Indicated for metastatic colorectal carcinoma, renal cell carcinoma, brain tumors, ovarian carcinoma, non-small cell lung cancer.
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trastuzumab
It is a monoclonal antibody against her-2/neu gene product.
it is useful for the treatment of breast carcinoma but cardiotoxicity limits its use.
Recently it is approved for the treatment of cancer of stomach and gastro-esophageal junction
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GnRH antagonists
Cetrorelix, ganirelix, degarelix and abarelix are the antagonists of LHRH.
These drugs decrease the release of gonadotropins without causing initial stimulation.
Degarelix has been approved for the treatment of prostatic carcinoma without the risk of flare reaction.
antiestrogens
Tamoxifen and toremifen are selective estrogen receptor modulators(SERMS)
that are useful for chemoprevention as well as treatment of both early stage and metastatic breast carcinoma.
These can lead to transient flare up reaction, menopausal symptoms and other estrogenic adverse effects
fulvestrant
Fulvestrant is a pure ER antagonist SERD(selective estrogen receptor down regulator)
having improved safety profile, faster onset and long duration.
Indicated for metastatic breast cancer
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aromatase inhibitors
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Second generation: formestane, fadrozole, rogletimide.
Third generation: letrozole, anastrozole, exemestane and vorozole.
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side effects of SERMs
Menopausal symptoms, fluid retention, thromboembolism and increased incidence of endometrial cancer.
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L-asparginase
It is an enzyme used for treatment of leukemias and lymphomas.
These tumors requires exogenous asparagine for growth.
L-asparaginase acts by depleting the aminoacid in the serum.
Administered by IV route. May cause severe hypersensitivity reactions, acute pancreatitis and cortical vein thrombosis.
uses of hydroxyurea
Used in sickle cell anemia, essential thrombocytosis and polycythemia vera, used in CML
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