SH-1028 + itraconazole

**SH-1028 + itraconazole** is a combination therapy consisting of SH-1028 (rilertinib), an irreversible third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI), and itraconazole, a triazole class antifungal drug that also functions as a potent CYP3A4 inhibitor. SH-1028 selectively targets EGFR mutations, including sensitizing and resistant (T790M) mutations, in locally advanced or metastatic non-small cell lung cancer (NSCLC). The combination is studied mainly to evaluate drug-drug interactions relevant for clinical use. Itraconazole inhibits CYP3A4, a key enzyme in SH-1028 metabolism, thereby affecting its pharmacokinetics and requiring dose management if co-administered. SH-1028 was developed to improve selectivity for EGFR mutant cells and mitigate side effects such as rash and diarrhea seen with other EGFR TKIs[1][2][3][6].

Brand names

Sanrisso

Other names

SH-1028SH1028SH 1028rilertinibSanrissoitraconazole