Orserdu

Monotherapy for postmenopausal women, & men, w/ estrogen receptor (ER) +ve, HER2 -ve, locally advanced or metastatic breast cancer w/ activating ESR1 mutation who have disease progression following at least 1 line of endocrine therapy including a CDK 4/6 inhibitor.

345 mg (one 345-mg tab) once daily. Continue treatment as long as clinical benefit is observed or until unacceptable toxicity occurs. Max daily dose: 345 mg. Concomitant use w/ strong CYP3A4 inhibitor 86 mg once daily. Concomitant use w/ moderate CYP3A4 inhibitor 172 mg once daily. Consider reducing to 86 mg once daily based on tolerability. Patient w/ moderate hepatic impairment (Child-Pugh B) Reduce dose to 258 mg (three 86-mg tab) once daily.

Should be taken with food: Swallow whole, do not chew/crush/split. Take at approx the same time each day. Administer w/ a light meal to reduce nausea & vomiting.

Hypersensitivity.

Consider risk of thromboembolic events when prescribing to patients at risk. Avoid concomitant administration w/ strong CYP3A4 inhibitors including clarithromycin, indinavir, itraconazole, ketoconazole, lopinavir/ritonavir, nefazodone, nelfinavir, posaconazole, saquinavir, telaprevir, telithromycin, voriconazole, & grapefruit or grapefruit juice; w/ moderate CYP3A4 inhibitors including aprepitant, ciprofloxacin, conivaptan, crizotinib, cyclosporine, diltiazem, dronedarone, erythromycin, fluconazole, fluvoxamine, grapefruit juice, imatinib, isavuconazole, tofisopam & verapamil; w/ strong CYP3A4 inducers including phenytoin, rifampicin, carbamazepine & St. John's wort; & w/ moderate CYP3A4 inducers including bosentan, cenobamate, dabrafenib, efavirenz, etravirine, lorlatinib, phenobarb, primidone & sotorasib. Concomitant use w/ OATP2B1 inhibitors. Observe caution in patients who experience fatigue, asthenia, & insomnia when driving or operating machinery. Patients w/ hepatic impairment; regularly & closely monitor these patients for adverse reactions. Not recommended in patients w/ severe hepatic impairment (Child-Pugh C). Has not been studied in patients w/ severe renal impairment. Not to be used during pregnancy or in women of childbearing potential not using contraception. Advise females of reproductive potential to use effective contraception during treatment & 1 wk after the last dose. Inform patient of the potential hazard to the foetus & potential risk of miscarriage if pregnancy occurs while taking Orserdu. Lactation; recommend lactating women not to breastfeed during treatment & 1 wk after the last dose. May impair fertility in females & males of reproductive potential. Safety & efficacy have not been established in childn from birth to 18 yr. Limited data are available in patients ≥75 yr.

Anaemia; decreased appetite; headache; hot flush; nausea, vomiting, diarrhoea, constipation, abdominal pain, dyspepsia; arthralgia, back pain; fatigue; increased AST, triglycerides, cholesterol, ALT & creatinine, & decreased Ca, Na & K. UTI; decreased lymphocyte count; insomnia; dizziness, syncope; dyspnoea, cough; stomatitis; rash; pain in extremity, musculoskeletal chest & bone pain; asthenia; increased blood alkaline phosphatase.

Increased AUC_inf & C_max w/ strong CYP3A4 inhibitors (eg, itraconazole). Increased steady-state AUC & C_max w/ moderate CYP3A4 inhibitors (eg, fluconazole, erythromycin). Decreased AUC_inf & C_max w/ strong CYP3A4 inducers (eg, rifampicin). Decreased steady-state AUC & C_max w/ moderate CYP3A4 inducers (eg, efavirenz). Increased exposure w/ OATP2B1 inhibitors. Increased exposure of digoxin & other P-gp substrates; rosuvastatin & other BCRP substrates.

Targeted Cancer Therapy

L02BA04 - elacestrant ; Belongs to the class of anti-estrogens. Used in treatment of neoplastic diseases.

POM