©THEBRIGHTSTARS 2024
PMCOL 344 Cancer Exam Study Guide.
Nucleobases - answer✔Purine analogs that are converted into fake nucleotides that get
incorporated into DNA and inhibit various enzymes.
Camptothecin - answer✔Topoisomerase 1B inhibitor that forms a stable tertiary complex with
TI-DNA complex. Causes DNA strand breaks that result in apoptosis. However, low blood
solubility.
Irinotecan - answer✔Semisynthetic analogue of camptothecin to improve solubility while
retaining cytotoxicity. Topoisomerase 1B inhibitor that forms a stable tertiary complex with TI-
DNA complex. Causes DNA strand breaks that result in apoptosis. Prodrug that is converted to
its active form by carboxyl esterase. Inactivated by UGT1A1 and CYP3A4.
FOLFIRI - answer✔5-fluorouracil, leucovorin, irinotecan -> for colon cancer.
Topotecan - answer✔Semisynthetic analogue of camptothecin to improve solubility while
retaining cytotoxicity. Topoisomerase 1B inhibitor that forms a stable tertiary complex with TI-
DNA complex. Causes DNA strand breaks that result in apoptosis.
Rubicins - ALL (adriamycin) - answer✔Anthracyclin - inhibits TI II (subtype independent) and
causes DNA strand breaks. Intercalative binding to DNA which partially unwinds DNA (but
tightly packed DNA not sensitive to this). Cell cycle non-specific. Formation of free radicals
(DNA strand breaks and cell membrane damage). Dose limiting myelosuppression and mucositis
(GI). Also cardiac toxicity but mechanism is delayed + cumulative over life.
Dexrazoxone - answer✔TI II inhibitor that reduced adverse cardiac effects in women on
Rubicins -> iron chelator (antioxidant), usually co-administered with carvedilol (adrenoreceptor
blocker) which is an antioxidant in cardiac tissue.
Mitoxantron - answer✔Anthraquinone that acts like anthracyclines but with fewer toxicities.
Pixantrone - answer✔Anthraquinone that acts like anthracyclines but with fewer toxicities.
Etoposide - answer✔Podophyllotoxin derivative, non-intercalating inhibitor of TI II, forms a
stable tertiary complex with TI II-DNA, causes ss and ds breaks. Specific to late S and early G2
phase. Dose limiting myelosuppression.
, ©THEBRIGHTSTARS 2024
Teniposide - answer✔Podophyllotoxin derivative, non-intercalating inhibitor of TI II, forms a
stable tertiary complex with TI II-DNA, causes ss and ds breaks. Specific to late S and early G2
phase. Dose limiting myelosuppression. Better cell accumulation than etoposide.
Vincristine (CHO) - answer✔Vinca alkaloids - binds to tubulin at the end of MTS and dimers,
prevents assembly of MTs (destabilizes) and causes dissolution of mitotic spindles, inhibits
organelle transport (esp in mitochondria of neural cells). Specific to G1/S phase. Dose limiting
peripheral neuropathy.
Vinblastine (CH3) - answer✔Vinca alkaloids - binds to tubulin at the end of MTS and dimers,
prevents assembly of MTs (destabilizes) and causes dissolution of mitotic spindles, inhibits
organelle transport (esp in mitochondria of neural cells). Specific to G1/S phase. Dose limiting
myelosuppression.
Paclitaxel - answer✔Taxol, binds to tubulin and enhances its polymerization (stabilizer),
inhibits cell replication and is specific to G2/M phase.
Docetaxel - answer✔Taxol, binds to tubulin and enhances its polymerization (stabilizer),
inhibits cell replication and is specific to G2/M phase. Higher affinity for tubulin binding site
than paclitaxel. Dose limiting myelosuppression. Can cause hypersensitivity r reactions.
Noscapine - answer✔Isoquinoline alkaloid that agonizes sigma opioid receptor. Can be used as
a non-sedating antitussive but is being investigated for cancers bc fewer side effects than other
MT disruptors. Also a poor substrate for efflux transporters.
Tamoxifen - answer✔SERM (for cancer). Competitive inhibitor of ER in breast tissue (used in
ER+ and PR+ breast cancer), prophylactic treatment for high risk ppl. Prodrug metabolized by
CYP2D6. Side effects include hot flashes, endometrial cancer (due to agonistic effects one
receptors in the uterus), thromboembolic events, depression. SSRIs interfere with CYP2D6
activity and reduces effectiveness.
Raloxifen - answer✔SERM (for cancer). Competitive inhibitor of ER in breast tissue and in the
uterus. Agonist effects in bone to treat osteoporosis in menopausal women. Only effective in
ER+ cancers.
Anastrazole - answer✔Second-line hormonal therapy for breast cancer, selective aromatase
inhibitor so can't produce estrogen.
Leuprolide - answer✔Medical castration - GnRH agonist that essentially desensitizes pituitary
so it stops releasing LHRH, decreasing T production. Initial T flare before sensitization.
Degarelix - answer✔GnRH antagonist for prostate cancer. Decreases T production, no flare.
Abiraterone - answer✔Androgen synthesis inhibitor. Inhibits CYP17A1 (so prevents
production of pregnenolone and progesterone to their 17-a derivatives, and the formation of
DHEA and androstenedione!). Used in castration-resistant prostate cancer.
PMCOL 344 Cancer Exam Study Guide.
Nucleobases - answer✔Purine analogs that are converted into fake nucleotides that get
incorporated into DNA and inhibit various enzymes.
Camptothecin - answer✔Topoisomerase 1B inhibitor that forms a stable tertiary complex with
TI-DNA complex. Causes DNA strand breaks that result in apoptosis. However, low blood
solubility.
Irinotecan - answer✔Semisynthetic analogue of camptothecin to improve solubility while
retaining cytotoxicity. Topoisomerase 1B inhibitor that forms a stable tertiary complex with TI-
DNA complex. Causes DNA strand breaks that result in apoptosis. Prodrug that is converted to
its active form by carboxyl esterase. Inactivated by UGT1A1 and CYP3A4.
FOLFIRI - answer✔5-fluorouracil, leucovorin, irinotecan -> for colon cancer.
Topotecan - answer✔Semisynthetic analogue of camptothecin to improve solubility while
retaining cytotoxicity. Topoisomerase 1B inhibitor that forms a stable tertiary complex with TI-
DNA complex. Causes DNA strand breaks that result in apoptosis.
Rubicins - ALL (adriamycin) - answer✔Anthracyclin - inhibits TI II (subtype independent) and
causes DNA strand breaks. Intercalative binding to DNA which partially unwinds DNA (but
tightly packed DNA not sensitive to this). Cell cycle non-specific. Formation of free radicals
(DNA strand breaks and cell membrane damage). Dose limiting myelosuppression and mucositis
(GI). Also cardiac toxicity but mechanism is delayed + cumulative over life.
Dexrazoxone - answer✔TI II inhibitor that reduced adverse cardiac effects in women on
Rubicins -> iron chelator (antioxidant), usually co-administered with carvedilol (adrenoreceptor
blocker) which is an antioxidant in cardiac tissue.
Mitoxantron - answer✔Anthraquinone that acts like anthracyclines but with fewer toxicities.
Pixantrone - answer✔Anthraquinone that acts like anthracyclines but with fewer toxicities.
Etoposide - answer✔Podophyllotoxin derivative, non-intercalating inhibitor of TI II, forms a
stable tertiary complex with TI II-DNA, causes ss and ds breaks. Specific to late S and early G2
phase. Dose limiting myelosuppression.
, ©THEBRIGHTSTARS 2024
Teniposide - answer✔Podophyllotoxin derivative, non-intercalating inhibitor of TI II, forms a
stable tertiary complex with TI II-DNA, causes ss and ds breaks. Specific to late S and early G2
phase. Dose limiting myelosuppression. Better cell accumulation than etoposide.
Vincristine (CHO) - answer✔Vinca alkaloids - binds to tubulin at the end of MTS and dimers,
prevents assembly of MTs (destabilizes) and causes dissolution of mitotic spindles, inhibits
organelle transport (esp in mitochondria of neural cells). Specific to G1/S phase. Dose limiting
peripheral neuropathy.
Vinblastine (CH3) - answer✔Vinca alkaloids - binds to tubulin at the end of MTS and dimers,
prevents assembly of MTs (destabilizes) and causes dissolution of mitotic spindles, inhibits
organelle transport (esp in mitochondria of neural cells). Specific to G1/S phase. Dose limiting
myelosuppression.
Paclitaxel - answer✔Taxol, binds to tubulin and enhances its polymerization (stabilizer),
inhibits cell replication and is specific to G2/M phase.
Docetaxel - answer✔Taxol, binds to tubulin and enhances its polymerization (stabilizer),
inhibits cell replication and is specific to G2/M phase. Higher affinity for tubulin binding site
than paclitaxel. Dose limiting myelosuppression. Can cause hypersensitivity r reactions.
Noscapine - answer✔Isoquinoline alkaloid that agonizes sigma opioid receptor. Can be used as
a non-sedating antitussive but is being investigated for cancers bc fewer side effects than other
MT disruptors. Also a poor substrate for efflux transporters.
Tamoxifen - answer✔SERM (for cancer). Competitive inhibitor of ER in breast tissue (used in
ER+ and PR+ breast cancer), prophylactic treatment for high risk ppl. Prodrug metabolized by
CYP2D6. Side effects include hot flashes, endometrial cancer (due to agonistic effects one
receptors in the uterus), thromboembolic events, depression. SSRIs interfere with CYP2D6
activity and reduces effectiveness.
Raloxifen - answer✔SERM (for cancer). Competitive inhibitor of ER in breast tissue and in the
uterus. Agonist effects in bone to treat osteoporosis in menopausal women. Only effective in
ER+ cancers.
Anastrazole - answer✔Second-line hormonal therapy for breast cancer, selective aromatase
inhibitor so can't produce estrogen.
Leuprolide - answer✔Medical castration - GnRH agonist that essentially desensitizes pituitary
so it stops releasing LHRH, decreasing T production. Initial T flare before sensitization.
Degarelix - answer✔GnRH antagonist for prostate cancer. Decreases T production, no flare.
Abiraterone - answer✔Androgen synthesis inhibitor. Inhibits CYP17A1 (so prevents
production of pregnenolone and progesterone to their 17-a derivatives, and the formation of
DHEA and androstenedione!). Used in castration-resistant prostate cancer.
