Rx Flashcards
<p>Imiquimod</p>
<p><strong>TLR7 agonist</strong></p>
<ul> <li>used in BCC, actinic keratosis, genital warts</li> <li>potent immune stimulator <ul> <li>activates <ul> <li>Langerhans cells in the skin</li> <li>macrophages</li> <li>NK</li> <li>BCs</li> </ul> </li> <li>secretion of <ul> <li>IFN-α</li> <li>IL-6</li> <li>TNF-α</li> </ul> </li> </ul> </li></ul>
<p>Nivolumab</p>
<p><strong>PDL-1 blocker (PD-1 antagonist)</strong></p>
<ul> <li>fully human IgG4 anti-PD1 mAb</li> <li>checkpoint inhibitor <ul> <li>blocks PDL-1 signalling that would have induced TCs to die and prevented them from attacking cancer cells</li> </ul> </li> <li>part of 2018 Nobel Prize in Physiology/Medicine (Honjo)</li></ul>
<p>Ipilimumab</p>
<p><strong>CTLA-4 antagonist</strong></p>
<ul> <li>fully human IgG1 anti-CTLA-4 mAb <ul> <li>binds CTLA-4 to prevent regulatory signalling to TCs by APC CD80/CD86</li> </ul> </li> <li>part of 2018 Nobel Prize in Physiology/Medicine (Allison)</li></ul>
<p>Abatacept</p>
<p><strong>CTLA4-Ig (competitively binds to co-stim CD80/CD86 to prevent TC co-receptor CD28 from binding, prevents signal 2)</strong></p>
<ul> <li>IgG1 fusion protein: CTLA-4 EC receptor domain + modified IgG1 Fc <ul> <li>decreases immune activation</li> </ul> </li> <li>binds CD80/86 co-stimulation and blocks binding of CD28 on TCs</li></ul>
<p>Etanercept</p>
<p><strong>Anti-TNF blocker</strong></p>
<ul> <li>TNF-R IgG1 fusion protein</li> <li>binds to and inactivates TNF</li></ul>
<p>Biologic/targeted therapies for RA (6)</p>
<ol> <li>Anti-TNF (5)</li> <li>Anti-BC (rituximab)</li> <li>Anti-TC (CTLA4-Ig)</li> <li>Anti-IL-6R</li> <li>Anti-macrophage (Ab against GM-CSF receptor)</li> <li>Targeted synthetic DMARDs (SMIs)</li></ol>
<p>sipuleucel-T (Provenge)</p>
<ul> <li>cellular cancer therapy</li> <li>DCs + TCs</li> <li>treatment of advanced CaP</li></ul>