entrectinib (Rozlytrek)

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Indications

ROS1-positive metastatic non-small cell lung cancer (NSCLC)
solid tumors with neurotrophic tyrosine receptor kinase (NTRK) gene fusion
orphan drug designation for treatment of neuroblastoma
orphan drug designation for treatment of TrkA-, TrkB-, TrkC-, ROS1- & ALK-positive non-small cell lung cancer (NSCLC) & metastatic colorectal cancer

Dosage

600 mg PO QD

Tabs: 100 mg, 200 mg

Adverse effects

most common (>= 20%):
- fatigue, constipation, dysgeusia, edema, dizziness, diarrhea, nausea, dysesthesia, dyspnea, myalgia, cognitive impairment, increased weight, cough, vomiting, pyrexia, arthralgia, visual impairment
serious:
- congestive heart failure, central nervous system dysfunction, bone fractures, hepatotoxicity, hyperuricemia, QT prolongation, visual impairment

Mechanism of action

ALK inhibitor

More general terms

small inhibitory antineoplastic agent (ib drug)

References

↑ RxNorm
↑ Wikipedia: Entrectinib https://en.wikipedia.org/wiki/Entrectinib
↑ FDA News Release. Aug 15, 2019. FDA approves entrectinib for NTRK solid tumors and ROS-1 NSCLC https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-entrectinib-ntrk-solid-tumors-and-ros-1-nsclc
↑ Highlight of Prescribing Information https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212725s000lbl.pdf

Database

PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid= 25141092

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