Bladder, kidney, and other urologic cancers:

Indications for INLYTA:

In combination with avelumab or pembrolizumab for first-line treatment of advanced renal cell carcinoma (RCC). As a single agent for the treatment of advanced RCC after failure of one prior systemic therapy.

Adult:

Take 12hrs apart. Swallow whole with a glass of water. First-line RCC: Initially 5mg twice daily in combination with avelumab (800mg IV infusion over 60mins every 2 weeks until disease progression or unacceptable toxicity); may escalate Inlyta dose at intervals of ≥2 weeks; or in combination with pembrolizumab (200mg every 3 weeks or 400mg every 6 weeks via IV infusion over 30mins until disease progression or unacceptable toxicity); may escalate Inlyta dose at intervals of ≥6 weeks. Second-line RCC: Initially 5mg twice daily. If tolerated for at least 2 consecutive weeks with no adverse reactions >Grade 2, normotensive, and not receiving antihypertensives, may increase dose to 7mg twice daily, then 10mg twice daily. If interruption, discontinuation, and/or dose reduction required: may reduce from 5mg twice daily to 3mg twice daily, and then 2mg twice daily if additional reduction required. Concomitant strong CYP3A4/5 inhibitors: avoid; if warranted, decrease Inlyta dose by approximately ½. If strong CYP3A4/5 inhibitor discontinued, return Inlyta dose (after 3–5 half-lives of the inhibitor) to that used prior to CYP3A4/5 inhibitor initiation. Moderate hepatic impairment: decrease dose by approximately ½. Dose modification for hepatotoxicity: see full labeling.

Children:

Not studied.

Warnings/Precautions:

Control and monitor BP prior to and during therapy; discontinue if severe and persistent hypertension (despite antihypertensive therapy and dose reduction). Risk of thromboembolic events. Untreated brain metastasis, recent active GI bleed: not recommended. Interrupt therapy if bleeding requires medical intervention. Monitor for cardiac failure during therapy; permanently discontinue if occurs. GI perforation and fistula formation; monitor. Monitor thyroid, liver function (ALT, AST, bilirubin), and for proteinuria before starting therapy, then periodically. Monitor for hepatotoxicity more frequently in combination treatments. Reduce dose or temporarily interrupt for moderate to severe proteinuria. Risk of reversible posterior leukoencephalopathy syndrome; discontinue if occurs. Impaired wound healing: withhold for ≥2 days prior to elective surgery; do not give for ≥2 weeks after major surgery and until adequate healing. In combination with avelumab: monitor for major adverse cardiovascular events; discontinue Inlyta/avelumab for Grade 3–4 events. ESRD. Severe hepatic impairment: not studied. Embryo-fetal toxicity. Advise females of reproductive potential and males (w. female partners) to use effective contraception during and for 1 week after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 2 weeks after the last dose).

Pharmacologic Class:

Kinase inhibitor.

Interactions:

See Adults. Avoid strong CYP3A4/5 inhibitors (eg, grapefruit juice, ketoconazole, itraconazole, clarithromycin, atazanavir, indinavir, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole), CYP3A4/5 inducers (eg, rifampin, dexamethasone, phenytoin, carbamazepine, rifabutin, rifapentin, phenobarbital, St. John’s wort), moderate CYP3A4/5 inducers (eg, bosentan, efavirenz, etravirine, modafinil, nafcillin).

Adverse Reactions:

Diarrhea, nausea, vomiting, hypertension, fatigue, decreased appetite, dysphonia, palmar-plantar erythrodysesthesia (hand-foot) syndrome, weight decreased, asthenia, constipation. In combination with avelumab: also musculoskeletal pain, mucositis, hypothyroidism, rash, hepatotoxicity, cough, dyspnea, abdominal pain, headache. In combination with pembrolizumab: also hepatotoxicity, stomatitis/mucosal inflammation, rash, cough.

Generic Availability:

NO

How Supplied:

Tabs 1mg—180; 5mg—60

Pricing for INLYTA

5mg tablet (Qty: 60)
Appx. price $15870
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