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Dermatology Pharmacology > Drugs to Treat Skin Cancers > Flashcards

Drugs to Treat Skin Cancers Flashcards

(36 cards)

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1
Q

Most skin cancers are cured if treated early, but not if they metastasize. Where does skin cancer commonly metastasize to?

A

Skin cancer typically metastasizes to:
• Intestines
• Lungs
• Brain

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2
Q

What drugs are used in the treatment of Basal Cell Carcinoma? (name 4)

A
  • Aminolevulinic Acid
  • Porfimer
  • Sonidegib
  • Vismodegib
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3
Q

What drugs are used in the treatment of Squamous Cell Carcinoma?

A
  • Aminolevulinic Acid
  • Afatinib
  • Cetuximab
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4
Q

What is the problem with Hedgehog Signaling that leads to cancer?
• what cancers does this most often lead to?

A

Dysregulation in Hedgehog signaling may lead to basal cell carcinomas, medulloblastomas, and rhabdomyosarcomas.

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5
Q

What is the biochemistry behind why Hedgehog Signaling leads to Cancer?
• Where do we have to block this pathway if we want to inhibit it?

A

Upregulation of Bcl-2 (anti-apoptotic) and VEGF (angiogenesis) are two important causes of cancer

If we want to inhibit this pathway then we must block AT or BELOW the level of the SMO transmembrane protein because the SMO transmembrane protein can stimulate the pathway independent of ligand binding.

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6
Q

Would blocking PTCH 1 be an effective way to go about blocking the Hedgehog pathway?

A

NOOO, this receptor is before the SMO receptor

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7
Q

What general statements can be made about the toxicity of Targeted Drugs? (2 generalizations)
• what can we do to help prevent this?

A
  1. Targeted drugs ironically affect every organ system in the body
  2. Cumulative Toxicity is a common event

Surveillance and early management is key to preventing symptoms

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8
Q

What is Actinic Keratosis?
• Where is it most commonly seen?
• what are the chances that it will develop into cancer if left untreated?
• What kind of cancer?

A

Actinic Keratosis is a scaly, crusty growth caused by UV damage. These pop up in heavily sun exposed areas of the body. If left untreated less than 10% develop into Squamous Scale Carcinoma.

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9
Q

What targeted Drugs are used in the treatment of Actinic Keratosis?

A

Diclofenac
Imiquimod
Ingenol Mebutate
Aminolevulinic Acid
Methylaminolevulinic Acid

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10
Q

What are the symptoms of Vascular Leak syndrome?
• what melanoma fighting drug causes this?

A

VLS can result in hypotension, pulmonary edema, end-organ damage (LIVER and RENAL failure)

Aldesleukin can have this side effect

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11
Q

What is the role of CTLA-4 in the immune system?
• what drugs bind this?

A

For T-cell activation/recognition to occur MHC class I/II and CD 80/86 on APCs must bind TCR and CD28 respectively. Like CD28, CTLA-4 also binds CD 80/86 but it prevents T-cell activation.

• Ipilumumab - binds and prevents CTLA-4 from inhibiting immune response - increases immune surveillance

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12
Q

What is the role of PDL1 in the immune system?
​• what drugs bind this?

A

PDL1 is a ligand on cells that can bind to PD1 on Tcells to decrease immune surveillance

* Nivolumab and Pembolizumab bind this

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13
Q

When is CTLA-4 most highly expressed?

A

CTLA-4 is expressed most strongly in strong immune responses, this helps tone down the body’s immune response to an antigen.

**Note: Niave Tcells do not express CTLA-4, instead it is sequestered in vesicles and is release AFTER TCR stimulation. The amount expressed on the surface is in proportion to the strenght of TCR-MHC interaction

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14
Q

When is PD-1 most highly expressed and what is its role?

A

PD-1 is most highly expressed in inflammation. It’s expressed by our own cells in peripheral tissues to keep our immune cells from attacking us

***when our cells sense IFN-gamma they know to upregulate PD1 expression

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15
Q

What transduction inhibitors work to inhibit BRAF?

A
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16
Q

What transduction inhibitors work to inhibit MEK1/2?

17
Q

What drugs require genotyping before you administer them?

Study These Flashcards
A

BRAF V600E drugs: Dabrafenib, Vemurafenib

18
Q

Aminolevulinic Acid

Administration

MOA

INDICATION

SIDE EFFECTS

CONTRAINDICATIONS

GENOTYPING

Study These Flashcards
A

Aminolevulinic Acid

MOA

Applied topically and acts as a prodrug for protoporphyrin IX. Light excitation of this drug in the presence of O2 leads to a cytotoxic reaction

INDICATION
Basal Cell Carcinoma AND Squamous Cell Carcinoma AND Actinic Keratosis

SIDE EFFECTS – not mentioned

CONTRAINDICATIONS – not mentioned

GENOTYPING – not mentioned

19
Q

Porfimer

Administration

MOA

INDICATION

SIDE EFFECTS

CONTRAINDICATIONS

GENOTYPING

Study These Flashcards
A

Porfimer

MOA

Applied topically. It get retained by tumor cells. Light excitation then produces FREE RADICALS in the cell.

INDICATION
Basal Cell Carcinoma

SIDE EFFECTS – not mentioned

CONTRAINDICATIONS – not mentioned

GENOTYPING – not mentioned

20
Q

Vismodegib

Administration

MOA

INDICATION

SIDE EFFECTS

CONTRAINDICATIONS

GENOTYPING

Study These Flashcards
A

Sonidegib/Vismodegib

Administratoin
Oral

MOA
Inhibition of SMO in the sonic hedgehog pathway

INDICATION
Basal Cell Carcinoma

SIDE EFFECTS
Extensive CYP metabolism
VERY COMMON – alopecia, GI toxicity, inc. in Creatinine, Endocrine dysfunction

CONTRAINDICATIONS
PREGNANCY – females AND MALES (toxic semen) need protection during and 20 mo.(F) or 8 mo.(M) after therapy
Renal dysfunction – RFTs need to be routine

GENOTYPING – not mentioned

21
Q

Sonidegib

Administration

MOA

INDICATION

SIDE EFFECTS

CONTRAINDICATIONS

GENOTYPING

Study These Flashcards
A

Sonidegib/Vismodegib

Administratoin
Oral

MOA
Inhibition of SMO in the sonic hedgehog pathway

INDICATION
Basal Cell Carcinoma

SIDE EFFECTS
Extensive CYP metabolism
VERY COMMON – alopecia, GI toxicity, inc. in Creatinine, Endocrine dysfunction

CONTRAINDICATIONS
PREGNANCY – females AND MALES (toxic semen) need protection during and 20 mo.(F) or 8 mo.(M) after therapy
Renal dysfunction – RFTs need to be routine

GENOTYPING – not mentioned

22
Q

Afatinib

Administration

MOA

INDICATION

SIDE EFFECTS

CONTRAINDICATIONS

GENOTYPING

Study These Flashcards
A

Afatinib
Administration – Oral

MOA
Irreversible TKI of EGFR (ErbB1) and HER2 (ErbB2) resulting in reduced ErbB signaling and proliferation

INDICATION
Squamous Cell Carcinoma

SIDE EFFECTS

Numerous. CYP metabolism => Hepatic Dysfunction
Renal Dysfunction

SEVERE RASH

CONTRAINDICATIONS – not mentioned

GENOTYPING – not mentioned

23
Q

Cetuximab

Administration

MOA

INDICATION

SIDE EFFECTS

CONTRAINDICATIONS

GENOTYPING

Study These Flashcards
A

Cetuximab
Administration – IV or SC

MOA
EGFR monoclonal antibody blocking phosphorylation and activation of receptor kinases (like RAS, RAF, MEK/ERK).

INDICATION

Squamous Cell Carcinoma

SIDE EFFECTS
• Numerous. EGFR TKIs are known to produce DERMATOLOGIC TOXICITY (Epithelial GFR) leading to dry skin, rash, pruritis
• GI toxicity
• CV toxicity (rare)

CONTRAINDICATIONS– not mentioned

GENOTYPING– not mentioned

24
Q

Iminquimod

Administration

MOA

INDICATION

SIDE EFFECTS

CONTRAINDICATIONS

GENOTYPING

Study These Flashcards
A

Iminquimod
Administration - Topical

MOA

Small molecule that induces tumor-directed immune response via Toll-like receptors leading to increased cytokines and Th1 immune response

INDICATION

Actinic Keratosis, Genital Warts

SIDE EFFECTS
Topical so localized to the skin and include: erythema, prurtis, peeling, burning at application site

CONTRAINDICATIONS
Compromises Condom and Diaphragm integrity when used to treat genital warts

Avoid sun exposure on Treated areas

GENOTYPING – not mentioned

25
**_Ingenol Mebutate_** _Administration_ _MOA_ _INDICATION_ _SIDE EFFECTS_ _CONTRAINDICATIONS_ _GENOTYPING_
**_Ingenol Mebutate_** _Administration_ – **Topical** _MOA_ Biphasic effect: 1. **Rapid lesion necrosis** (1-2 hrs after application) 2. **Neutrophil mediated ADCC** (days after application – b/c you have to make abs.) _INDICATION_ **Actinic Keratosis** _SIDE EFFECTS_ **Localized to Skin** b/c its topical. Includes: redness, swelling, **peeling of skin, pustular vasculitis, superficial ulceration** _CONTRAINDICATIONS_ _GENOTYPING_
26
**_Aldesleukin (IL-2)_** _Administration_ _MOA_ _INDICATION_ _SIDE EFFECTS_ _CONTRAINDICATIONS_ _GENOTYPING_
**_Aldesleukin (IL-2)_** _Administration_ – IV or SC _MOA_ **Give in HIGH dose which ACTIVATES effector T cells b/c its IL-2**_. In low doses this activates Treg cells and blocks immune response._ _INDICATION_ **Melanoma** _SIDE EFFECTS_ * **VLS (vascular leak syndrome)** triggered by binding of IL-2 to receptors on endothelium * **Impaired Neutrophil Function** leading to disseminated infection * Lethargy/Coma * ANY ORGAN SYSTEM COULD BE AFFECTED _CONTRAINDICATIONS_ Do not give to anyone with: Pre-existing infection, CV or Renal Problems _GENOTYPING_ - not mentioned
27
**_BCG Vaccine_** _Administration_ _MOA_ _INDICATION_ _SIDE EFFECTS_ _CONTRAINDICATIONS_ _GENOTYPING_
**_BCG Vaccine_** _Administration_ _MOA_ – TB vaccine given to prevent melanoma _INDICATION_ _SIDE EFFECTS_ _CONTRAINDICATIONS_ _GENOTYPING_
28
**_(Peg)Interferon-alpha-2B_** _Administration_ _MOA_ _INDICATION_ _SIDE EFFECTS_ _CONTRAINDICATIONS_ _GENOTYPING_
**_(Peg)Interferon-alpha-2B_** _Administration_ – IV or SC _MOA_ In general act through **JAK-STAT** receptors that homodimerize, go to the nucleus promote transcription of lots of genes **Indirect Effect**: **Upregulation of cytotoxic cells**: T-cells, NK cells, Dendritic cells. Downregulation of Immune inhibitory cells like T-regs. **Direct Effect**: **Prevents tumor cell proliferation and promotes apoptosis** _INDICATION_ **Melanoma** _SIDE EFFECTS_ **LIFE THREATENING NEUROPSYCHIATRIC DISORDERS, autoimmune, ischemic, infectious disorders** **\*\*\*Check LFTs, CXRs, CBCs, ECGs for evidence of Toxicity routinely\*\*\*\*** _CONTRAINDICATIONS_ – not mentioned _GENOTYPING_ – not mentioned
29
**_Ipilumumab_** _Administration_ _MOA_ _INDICATION_ _SIDE EFFECTS_ _CONTRAINDICATIONS_ _GENOTYPING_
**_Ipilumumab_** _Administration_ _MOA_ **Bind to CTLA-4 to prevent suppression initial activating immune response** _INDICATION_ Melanoma, NSCLC _SIDE EFFECTS_ **Toxic epidermal necrolysis (TEN**) and **other autoimmune reactions** Rash, lethargy, and pruitis are most common \*\*\*THESE EFFECTS ARE MORE COMMON IN CTLA-4 DRUGS than PD1 drugs\*\*\*\*\* **BBW: ENDOCRINOPATHIES, DIARRHEA, PERIPHERAL NEPHROPATHY, RASH** _CONTRAINDICATIONS_ **Do NOT give this drug to pregnant women** _GENOTYPING_ – not mentioned
30
**_Nivolumab_** _Administration_ _MOA_ _INDICATION_ _SIDE EFFECTS_ _CONTRAINDICATIONS_ _GENOTYPING_
**_Nivolumab, Pembolizumab_** _Administration_ _MOA_ **Bind to PD1 to upregulate immunorecognition in periphery** _INDICATION_ Melanoma, NSCLC (nivolumab only) _SIDE EFFECTS_ **Toxic epidermal necrolysis (TEN**) and **other autoimmune reactions** Rash, lethargy, and pruitis are most common \*\*\*THESE EFFECTS ARE MORE COMMON IN CTLA-4 DRUGS than PD1 drugs\*\*\*\*\* **BBW: ENDOCRINOPATHIES, DIARRHEA, PERIPHERAL NEPHROPATHY, RASH** _CONTRAINDICATIONS_ **Do NOT give this drug to pregnant women** _GENOTYPING_ – not mentioned
31
**_Pembolizumab_** _Administration_ _MOA_ _INDICATION_ _SIDE EFFECTS_ _CONTRAINDICATIONS_ _GENOTYPING_
**_Nivolumab, Pembolizumab_** _Administration_ _MOA_ **Bind to PD1 to upregulate immunorecognition in periphery** _INDICATION_ Melanoma, NSCLC (nivolumab only) _SIDE EFFECTS_ **Toxic epidermal necrolysis (TEN**) and **other autoimmune reactions** Rash, lethargy, and pruitis are most common \*\*\*THESE EFFECTS ARE MORE COMMON IN CTLA-4 DRUGS than PD1 drugs\*\*\*\*\* **BBW: ENDOCRINOPATHIES, DIARRHEA, PERIPHERAL NEPHROPATHY, RASH** _CONTRAINDICATIONS_ **Do NOT give this drug to pregnant women** _GENOTYPING_ – not mentioned
32
**_Cobitmetinib_** _Administration_ _MOA_ _INDICATION_ _SIDE EFFECTS_ _CONTRAINDICATIONS_ _GENOTYPING_
**_Cobitmetinib, Trametinib_** _Administration_ - Oral _MOA_ **MEK1 and MEK 2 blockade** _INDICATION_ Melanoma _SIDE EFFECTS_ **CYP3A4** associated effects and **P-glycoprotein** associated effects May be **affected by meal, PPIs** Toxicity profile may change on the basis of **SNPs and UGT1A/A19** Rash, CV problems, Pulmonary fibrosis, endicrinopathies, **corneal perforation** _CONTRAINDICATIONS_ – not mentioned _GENOTYPING_ – not mentioned
33
**_Trametinib_** _Administration_ _MOA_ _INDICATION_ _SIDE EFFECTS_ _CONTRAINDICATIONS_ _GENOTYPING_
**_Cobitmetinib, Trametinib_** _Administration_ - Oral _MOA_ **MEK1 and MEK 2 blockade** _INDICATION_ Melanoma _SIDE EFFECTS_ **CYP3A4** associated effects and **P-glycoprotein** associated effects May be **affected by meal, PPIs** Toxicity profile may change on the basis of **SNPs and UGT1A/A19** Rash, CV problems, Pulmonary fibrosis, endicrinopathies, **corneal perforation** _CONTRAINDICATIONS_ – not mentioned _GENOTYPING_ – not mentioned
34
**_Vemurafenib_** _Administration_ _MOA_ _INDICATION_ _SIDE EFFECTS_ _CONTRAINDICATIONS_ _GENOTYPING_
**_Dabrafenib, Vemurafenib_** _Administration_ – Oral _MOA_ **Dabrafenib (BRAF V600E,K,F, and wild-type) Vemurafenib (only BRAF V600E)** _INDICATION_ Melanoma _SIDE EFFECTS_ **CYP3A4** associated effects and **P-glycoprotein** associated effects May be **affected by meal, PPIs** Toxicity profile may change on the basis of **SNPs and UGT1A/A19** Rash, CV problems, Pulmonary fibrosis, endicrinopathies, **corneal perforation** _CONTRAINDICATIONS_ – not mentioned _GENOTYPING_ – **REQUIRED to determined V600E mutation**
35
**_Dabrafenib_** _Administration_ _MOA_ _INDICATION_ _SIDE EFFECTS_ _CONTRAINDICATIONS_ _GENOTYPING_
**_Dabrafenib, Vemurafenib_** _Administration_ – Oral _MOA_ **Dabrafenib (BRAF V600E,K,F, and wild-type) Vemurafenib (only BRAF V600E)** _INDICATION_ Melanoma _SIDE EFFECTS_ **CYP3A4** associated effects and **P-glycoprotein** associated effects May be **affected by meal, PPIs** Toxicity profile may change on the basis of **SNPs and UGT1A/A19** Rash, CV problems, Pulmonary fibrosis, endicrinopathies, **corneal perforation** _CONTRAINDICATIONS_ – not mentioned _GENOTYPING_ – **REQUIRED to determined V600E mutation**
36
**_Sorafenib_** _Administration_ _MOA_ _INDICATION_ _SIDE EFFECTS_ _CONTRAINDICATIONS_ _GENOTYPING_
**_Sorafenib_** _Administration_ – Oral _MOA_ **Inhibits multiple intracellular and surface kinases** _INDICATION_ Melanoma _SIDE EFFECTS_ **CYP3A4** associated effects and **P-glycoprotein** associated effects May be **affected by meal, PPIs** Toxicity profile may change on the basis of **SNPs and UGT1A/A19** Rash, CV problems, Pulmonary fibrosis, endicrinopathies, **corneal perforation** _CONTRAINDICATIONS_ – not mentioned

Dermatology Pharmacology (11 decks)

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