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Oncology Therapeutics Random Flashcards

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1
Q

Etoposide

A

Topoisomerase 2
Usually 2nd Line (After poor radiotx response)
Binds to DNA topoisomeraise II complex
Used in Testicular and Lung
Arrest cell in G2/M Phase = More Radiosensitive

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2
Q

Topotecan

A 
Topoisomerase 1
Usually 2nd Line
Prevents torsional relief in DNA 
Prevents religation of DNA
Increases Radiotherapy sensitivity of DNA
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3
Q

Vemurafenib

A

Inhibits cell proliferation in the setting of BRAF Mutation.

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4
Q

COX2

A

iNDUCIBLE ISOFORM THAT ACTIVATES PROTAGLANDIN PRODUCTION IN INFLAMMATORY CELLS.

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5
Q

FOLFOX

A

Oxaliplatin + 5FU/LV

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6
Q

Chimeric mAb

A

Consist of Fab regions from another species combined with the Fc portion of a human antibody, resulting in a construct that is approximately two thirds human.

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7
Q

IHC HER2 Scoring

A

IHC Scoring of Tumour with immunohistochemestry between 0-3

FISH+/-

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8
Q

Doxorubicin

A

Anti-Tumour Antibiotic
BREAST, ENDOMETRIAL AND OVARIAN (+Some Childhood)
Isolated from Stropomyces SPP

4x MOA’s

  1. Topomerase II inhibition
  2. High Affinity DNA intercalation
  3. Alteration of Membrane Fluidity
  4. Superoxide free radical damage. (cardiotoxic!)

Activation is by hydrOXYlation – Hence Cardiotoxic.

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9
Q

Targeted regional therapy for CRC liver Mets?

A

Hepatic arterial infusion

Floxuridine

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10
Q

Vincristine

A 
Vinca Alkaloid
Mainly Leukaemia. 
Bind to tubulin, preventing microtubulin formation. 
M-Phase specific. 
NEUROTOXIC
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11
Q

Mechlorethamine

A

Alkylating Agent

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12
Q

Thyroglobulin

A

Measurement only clinically useful in assessing recurrence of thyroid Cancer.

Suppressed TSH + elevated thyroglobulin suggests disease recurrence

Post-treatment thyroglobulin should be low (

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13
Q

Role of BRAF

A

Post RAS protein involved in signalling for cell growth.

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14
Q

Chlorambucil

A

Alkylating Agent

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15
Q

a-fetoprotein (AFP)

A

Used as a tumour marker in Hepatocellular carcinoma (HCC)/hepatoblastoma in children. Essentially junior albumin. Also: Germ cell teratomas of the testes/ovaries

Levels >20 mg/L prompt further investigation
Levels >200 mg/L suggestive of HCC
Levels >400 mg/L diagnostic of HCC

Also elevated in:
Pregnancy
Infancy
Non-malignant liver conditions e.g. cirrhosis, hepatitis, cholestasis

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16
Q

Trastuzumab

A

Mab against Her2 cell surface receptor
(binds to the extracellular domain of ERB2. Preventing extracellular activation of HER2 and signalling and flags cells for destruction by the imune system. Immune cells bind to trastuzumab and induce anti-tumour effect)
HER2+ Breast Cancer (Ajuvent & Metastatic Disease)
HER2+ Gastric Cancer
IV or Subcut

S/E
Cardiotoxicity (not dose dependent, regular ECG’s, do NOT GIVE with ANTHRACYCLINE)

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17
Q

Mitoxantrone

A

Anti-Tumour Antibiotic

Isolated from Stropomyces SPP

4x MOA’s

  1. Topomerase II inhibition
  2. High Affinity DNA intercalation
  3. Alteration of Membrane Fluidity
  4. Superoxide free radical damage. (cardiotoxic!)

Activation is by hydrOXYlation – Hence Cardiotoxic.

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18
Q

Brentuximab Verdotin

A

Group Iib mAb (only one approved).
Hodgkin Lymphoma
Targets CD30 antigen expressed in the tumours
Conjugared to MMAE

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19
Q

Tu prefix

A

Tumour.

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20
Q

Human chorionic gonadotrophin (hCG)

A

Elevated levels in germ cell tumours e.g. seminoma, teratoma, choriocarcinoma

Sensitive tumour marker

Screening:
Patients with molar pregnancies followed up for 6 months
Rising levels in absence of new pregnancy are diagnostic

Response to therapy:
Good response to chemo: 40,000 IU/L plus risk factors

Monitor treatment/disease recurrence
hCG levels should normalise and remain low

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21
Q

Group III Biotherapeutics

A

Protein Vaccines

• Eg HPV vaccine for prevention of HPV infection and associated cancers.

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22
Q

Cetuximab

A

mAb against EGF receptor (Anti-EGFR)
EGFR activated critical survival and evasion pathways.
EGFR overexpressed in 85% of CRC Tumours
Colorectal cancer (nsc lung and scc of head and neck)

If patient have RASH = BETTER OUTCOME!
Skin toxicity

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23
Q

Pertuzumab

A

HER2+ Brest Cancer
Prevents Dimerisation of HER2
Inhibits ligand activated dimerisation.

HER2+ Breast Cancer (Investigational)

Abnormal LFT’s

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24
Q

Trastuzumab Emtansine (T-DM1)

A

Trastuzumab (increases the therapeutic window of DM1)
+ DM1 = Potent Cytotoxic (targets microtubules)
Requires Stable Linker to keep bound

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25
a'
Rat mAb
26
Group IV Biotherapeutics
Protein Diagnostics • Eg GHRH used to diagnose defective GH secretion. • Imaging agents for cancer – eg anti-PSA antibody used to detect prostate cancer
27
Gefitinib and Erlotinib
Small Molecule Kinase Inhibitors MOA: EGFR inhibitors Used in Non-responsive Non-Small Cell Lung Cancer
28
CVS risk of COX2 Inhibition.
MI, STROKE, VENOUS CLOTS. Disruption of PG12 TxA2 balance = prothrombotic. Best ine = paproxen.
29
COX2 inhibition S/E
CVS morbidity and mortality.
30
Key Mediators of Inflammation? Pathway that produces?
Prostaglandins. Produced by the cycloxygenase pathway. Inhibited mainly by NSAIDs
31
Epirubicin
Anti-Tumour Antibiotic Isolated from Stropomyces SPP 4x MOA's 1. Topomerase II inhibition 2. High Affinity DNA intercalation 3. Alteration of Membrane Fluidity 4. Superoxide free radical damage. (cardiotoxic!) Activation is by hydrOXYlation – Hence Cardiotoxic.
32
STOP and GO?
NOT GOOD, DECREASED SURVIVIAL
33
Bleomycin
Anti-Tumour Antibiotic LYMPHOMAS, GERM CELL CANCERS, H+Neck Cancers. Isolated from Stropomyces SPP 4x MOA's 1. Topomerase II inhibition 2. High Affinity DNA intercalation 3. Alteration of Membrane Fluidity 4. Superoxide free radical damage. (cardiotoxic!) Activation is by hydrOXYlation – Hence Cardiotoxic.
34
Imantinib
Small Molecule Kinase Inhibitors MOA: Bind Tyrosine Kinase LYMPHOMAS AND LEUKAEMIAS
35
Lapatinib
Small Molecule INTRACELLULAR Kinase Inhibitor Directly inhibits phosphorylation and activation of downstream pathways. HER2+ Breast Cancer (After progression Trastuzumab) S/E Rash
36
Methotrexate
Anti-Metabolites (– Folic Acid Antagonist) Cell Cycle Specific (S-Phase) Inhibits dihydrofolate reductase, depleteing tetrahydrofolate. TOXIC TO BONE MARROW – Combine w/Folinic Acid
37
Humanized antibodies
Consist of only the CDRs from the foreign mAb, and are about 95% human.
38
Colorectal mAb's
Cetuximab and Panitumumab | Bevacizumab
39
Irinotecan
Topoisomerase 1 Plant Alkaloid Usually 2nd Line MOA: prevents DNA unwinding by inhibiting topoisomerase 1, resulting in inhiition of both replication and transcription Increases Radiotherapy sensitivity of DNA TOXICITY = Steatohepatitis
40
Carbohydrate antigen 19-9 (CA 19-9)
Pancreatic Cancer Biomarker. Prognosis: high pre-operative levels associated with poorer outcome than lower pre-operative concentrations Recurrence: post-surgery considered with rising concentrations
41
Idarubicin
Anti-Tumour Antibiotic Isolated from Stropomyces SPP 4x MOA's 1. Topomerase II inhibition 2. High Affinity DNA intercalation 3. Alteration of Membrane Fluidity 4. Superoxide free radical damage. (cardiotoxic!) Activation is by hydrOXYlation – Hence Cardiotoxic.
42
Carbohydrate antigen 125 (CA 125)
CA 125 raised in 90% of patients with advanced ovarian cancer. Used in screening for women >50yo with symptoms. If serum CA 125 ≥ 35 IU/mL → ultrasound scan of the abdomen and pelvis If CA 125
43
Renal Effect of Prostaglandin/inhibition
Acute interstitial nephritis, haemodynamic nephritis. Often with nephrotic (heavy proteinuria) .
44
COX1
Constant Housekeeper - Inhibits acid synthesis - Increases Blood flow - Stimulates constriction and clotting
45
Naproxen
Long Acting Non-COX selective Propionic Acid
46
Cisplatin and Carboplatin
Platinum Analogues Reactive complex that cross links guanine units in DNA. Used in Ovarian and Tesisticular C CISPLATIN = MOST TOXIC = EMETIC, NEPHRO AND OTO Toxicity
47
Group I Biotherapeutics
Enzymes and Regulatory Proteins • Mainly relevant to endocrine & metabolic diseases & hemostasis • Eg insulin; growth hormone; alglucosidase alpha (Pompe disease); clotting factors viii and ix; fibrinogen
48
FOLFIRI
Irinotecan + 5FU/LV
49
NSAID Hypersensitivty
Ocular and nasal congestion Sever bronchospasm Anaphylaxis. Variety of skin reactions. (Stevens Johnson Syndrome)
50
Resection?
* Direct correlation between RR and resection rate * Tumour progression on ‘pre-operative’ chemotherapy = an independent poor prognostic factor even after potentially curative liver resection * Curative strategies should focus on hepatic resection rate as an end-point
51
Nomenclature of -mAb drugs
Prefix = Unique for each. 2nd part = Drug Disease Group orginially developed for. 3rd Part = Species the mAb was derived from, the first vowel occurring in the species name. End = mAb (monoclonal antibody).
52
FOLFOXIRI
Better than two.
53
xi
Chimeric
54
Cyclophosphamide
Alkylating Agent
55
Gemtuzumab Ozogamicin (Mylotarg)
Group II b mAb Targets Anti-CD33 in LYMPHOMA WITHDRAWN Die to Liver Tox
56
Adjuvant Chemotherapy
+20% Benefit in survivability v surgery alone.
57
Bevacizumab
Humanized mAb that binds VEGF (ANTI-VEGF) Colorectal cancer Long T1/2 ``` S/E Hypertension Albuminuria GI Perforation (1% risk, mech not fully understood) Arterial Thrombotic Events Impaired Wound Healing ``` Wound healing; bleeding; liver regeneration
58
Rituximab
Chimeric mAb against CD20 Non-Hodgkins lymphoma Also now RA
59
Entercept
TNF receptor–Fc fusion protein • A dimeric fusion protein between the soluble TNF-α receptor and Fc portion of human IgG1 • Used to treat moderate-severe RA and also severe polyarticular juvenile RA. • Basically a TNF antagonist • Very successful drug
60
Catecholamines as biomarker.
Mostly Pheochromocytoma MEN2a and MEN2b Von Hippel-Lindau syndrome Neurofribromatosis Familial paraganglioma 24 hour collection required in acid preservative for the measurement of adrenaline, noradrenaline and dopamine 2/3 collections if transient hypertension. 1 if hypertension.
61
Oxiplatin
Platinum Analogues Reactive complex that cross links guanine units in DNA. Derivative from Cisplatin Works by inhibiting DNA synthesis Accumulative toxicity = Neuropathy (Related to cold. Can result in laryngeal spasm due to nerve hypersensitivity, other examples include hand spasm when reaching into fridge) Toxicity = Sinusoidal dilatation and vascular injury
62
Predicts Recurrence after resection
FONG Score
63
DPD Deficiency
Autosomal recessive metabolic disorder Absent or significantly decreased activity of dihydropyrimidine dehydrogenase Means that the drug is not broken down and recirculated with high toxicity putting the patient in ICU. This deficiency is rare. Testing or this deficiency is not routine
64
'zu'
HumanIZED mAb
65
o'
Mouse mAb
66
Infliximab
Group II mAb that binds to and neutralizes TNF-α | Crohn’s disease and RA
67
Paclitaxel
Taxanes Western Yew Tree OR form Syn Doxetaxel MOA= Prevent Microtubules DISASSEMBLY. Therefore arrests cell in Mitosis/G2 Assoc w/ severe hypersenstivity.
68
Li prefix
Immune
69
Daunorubicin
Anti-Tumour Antibiotic Isolated from Stropomyces SPP 4x MOA's 1. Topomerase II inhibition 2. High Affinity DNA intercalation 3. Alteration of Membrane Fluidity 4. Superoxide free radical damage. (cardiotoxic!) Activation is by hydrOXYlation – Hence Cardiotoxic.
70
Busulfan
Alkylating Agent
71
Alkylating Agent MOA?
Alpha Side Chain Metabolically Activated Reactive Produce binds to DNA Causes read and replication errors
72
Calcitonin
Medullary thyroid carcinoma (MTC)
73
Vinblastine
``` Vinca Alkaloid Mainly Lymphoma + Testicular Cancer Bind to tubulin, preventing microtubulin formation. M-Phase specific. Myelosuppressive (BM activity down) ```
74
Multiple Myeloma
Monoclonal Protein in Increase amounts. intact Igs, Ig fragments and/or monoclonal FLCs Single Clone of Bcells Causes - M proteins in blood and urine - Excess light chain production and excretion. - Amyloidosis - Deregulation of clotting factors, hormones and chemicals DETECTION Proteins migrate in the electrical field according to their charge and mass Alpha proteins – alpha 1 antitrypsin, haptoglobin, alpha 2 macroglobulin, HDL Beta proteins – transferrin, LDL, C3 Gamma proteins – immunglobulins, fibrogen, CRP
75
Etorocoxib
Selective | Long Acting
76
HAMA response
mAbs are foreign proteins, resulting in immune recognition and anti-mAb production,
77
Capecitabine
* Pro-drug, oral * Converted to 5-FU by thymidine phosphorylase * Bioavailability of almost 100%
78
ErbB2 receptor signal pathways
``` PI3K = Cell Cycle + Survival MAPK = Proliferation ```
79
COX1 inhibition S/E
Stomach, platelet, kidney
80
Celecoxib
CO2 selective | Pyrazole.
81
Ibuprufen
Non COX Selective | Propionic acid
82
Ifosfamide
Alkylating Agent
83
i'
Primate
84
HER Receptors
``` HER2 = No Ligand HER3 = No kinase activity ``` HER2:3 dimers initiate the strongest mitogenic signalling. HER2:3 dimers can be ligand activated and HER2 can phosphorylate HER3's intracell cascade. = Multiple signal pathways = increase tumour proliferation.
85
Group II Biotherapeutics
Targeted Proteins (The NB's) • Further subdivides into o Group IIa – Interfering with a molecule or protein (preventing ligand binding) o Group IIb – Delivering other compounds or proteins (antibody drug conjugates, which target antibody expressed by a group of cancerous cells)
86
u'
Human
87
Complete response Chemo in CRC w/Liver Mets
You must still perform a resection of the affect liver area, since recurrence in the affected tissues is common, possibly due to the augmentation of the immuno-system with chemo. * Difficult for the surgeon to resect * Radiologic CR does NOT mean pathologic CR * Duration of ‘preoperative’ treatment is critical * HAI has been shown to be an independent predictor of pCR
88
6 MP (Mercaptopurine--> 6 Thioguanine)
Anti-Metabolites (-Purine Anatagonists) Cell Cycle Specific (S-Phase) Childhood Leukaemia Pro Drug (Mercap to Thioguanine)
89
Challenges of Biotherapaeutics?
Drug delivery very difficult Cost (& its ethical implications) o Biosimilars will help reduce this Immunogenicity problematic o e.g hemophilia patients may make antibodies to Factor VIII when it is replaced. Increased humanization now... Proteins are large molecules with both hydrophilic and hydrophobic character o Solubility o Route of administration o Distribution – entry into cells difficult o Stability – subject to degradation/ clearance o Post-translational modification nb for function PEGylation used to prolong absorption, decrease renal clearance, increase half- life and reduce immunogenicity of many proteins
90
Carcinoembryonic antigen (CEA)
200 kDa glycoprotein and plays a role in cell adhesion Elevated in most advanced adenocarcinomas: colorectal cancer but also tumours of pancreas, breast, lung Was used for screening CRC but not specific enough now. Used for monitoring rather than diagnosis e.g. CA 125 (ovarian), CA 19-9 (pancreatic), CA 15.3 (breast)
91
Sorafenib Pazopanib and sunitinib
vEGF inhibtors
92
Human mAb
Where the sequence is entirely human, can be generated in a number of ways including immunization of transgenic animals that have a human immune system, repertoire cloning, and other techniques.
93
Breast Cancer mAb's
Trastuzumab Pertuzumab T-DMI
94
5-FU (5-Fluorouracil)
Anti-Metabolite (Pyramiding Antagonist) Inhibits synthesis of Thymine (vital for DNA synth) Acts by irreversibly inhibiting thymidylate synthase Leucovorin enhanced binding of 5FU to its substrate (TS) Infusional better than bolus HDFL Very Short T1/2 Used widely in Solid Tumours TOXICITY = Hepatic steatosis
95
Ipilimumab
Anti-CTLA-4 Antibody, Preventing CTLA-4 from binding to B7 and inactivating the cytotoxic t-cell. i.e. Switches off the off switch of CTLs ``` Metastatic Melanoma (possibly, RCC, Prostate and Lung) ``` S/E: Colitis, Hepatits, Hypophysitis. Treat with: Corticosteroids and Anti-TNF antibody if refractory.
96
Melphalan
Alkylating Agent
97
Melanoma mAb's
Ipilimumab | Novolumab
98
Nivolumab
Anti-PD1 Anti-PD1 antibodies may be more relevant to unleash an anti-melanoma immune response than anti-CTLA4 antibodies

Oncology (5 decks)

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