Peringatan Keamanan

Toxicity information regarding elacestrant is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as dyslipidemia and gastrointestinal disorders.L44918 Symptomatic and supportive measures are recommended. The carcinogenicity of elacestrant has not been evaluated. Elacestrant did not show mutagenicity in the in vitro Ames assay and was negative for clastogenicity in in vitro chromosome aberration assays and the in vivo rat bone marrow micronucleus assay.L44918

Fertility studies with elacestrant in animals have not been performed. Rats and cynomolgus monkeys presented adverse reactions in female reproductive organs including atrophy of the vagina, cervix, and uterus and follicular cysts in the ovary after receiving repeated doses of elacestrant. Male rats presented decreased cellularity of Leydig cells and degeneration/atrophy of the seminiferous epithelium in the testis.L44918

Elacestrant

DB06374

small molecule approved investigational

Deskripsi

Elacestrant is a non-steroidal small molecule and an estrogen receptor (ER) antagonist.A256838,L44918 In January 2023, it was approved by the FDA for the treatment of ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer.L44918,L44948 It received a similar approval in the EU in September 2023.L49334

Elacestrant binds to estrogen receptor-alpha (ER?) and acts as a selective estrogen receptor degrader (SERD) thanks to its ability to block the transcriptional activity of the ER and promote its degradation.A256828,A256863,L44948 Other types of endocrine therapy, such as selective estrogen receptor modulators (SERMs) and aromatase inhibitors (AIs), may lead to drug resistance over time; therefore, the use of a SERD represents a therapeutic approach for the treatment of endocrine-resistant breast cancers.A256878 Unlike fulvestrant, another FDA-approved SERD, elacestrant is orally bioavailable.A256833

Struktur Molekul 2D

Berat 458.646
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of elacestrant is 30 to 50 hours.[L44918]
Volume Distribusi Elacestrant has an apparent volume of distribution of 5800 L.[L44918]
Klirens (Clearance) Elacestrant has an estimated clearance of 186 L/hr and a renal clearance of ? 0.14 L/hr.[L44918]

Absorpsi

With the recommended dosage of 345 mg once daily, elacestrant has a steady-state Cmax of 119 ng/mL and an AUC0-24h of 2440 ng?h/mL. The Cmax and AUC of elacestrant increase more than dose-proportional between 43 mg and 862 mg once daily (0.125 to 2.5 times the approved recommended dosage). By day 6, elacestrant reaches steady-state and has a 2-fold mean accumulation ratio based on AUC0-24h. The tmax of elacestrant goes from 1 to 4 hr, and its oral bioavailability is approximately 10%. Compared to a fasted state, the Cmax and AUC of elacestrant (345 mg) were 42% and 22% higher, respectively, when administered with a high-fat meal (800 to 1000 calories, 50% fat).L44918

Metabolisme

Elacestrant is metabolized in the liver, mainly by CYP3A4 and, to a lesser extent, by CYP2A6 and CYP2C9.L44918

Rute Eliminasi

Elacestrant is mainly eliminated through feces and urine. Approximately 82% was recovered in feces (34% unchanged), and 7.5% was recovered in urine (< 1% unchanged) following a single radiolabeled oral dose of 345 mg.L44918

Interaksi Makanan

1 Data
  • 1. Take with food. Take with food to reduce nausea and vomiting.

Interaksi Obat

351 Data
Darbepoetin alfa The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Elacestrant.
Erythropoietin The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Elacestrant.
Peginesatide The risk or severity of Thrombosis can be increased when Peginesatide is combined with Elacestrant.
Methoxy polyethylene glycol-epoetin beta The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Elacestrant.
Lidocaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Lidocaine.
Ropivacaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Ropivacaine.
Bupivacaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Bupivacaine.
Cinchocaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Cinchocaine.
Dyclonine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Dyclonine.
Procaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Procaine.
Prilocaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Prilocaine.
Proparacaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Proparacaine.
Meloxicam The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Meloxicam.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Oxybuprocaine.
Cocaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Cocaine.
Mepivacaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Mepivacaine.
Levobupivacaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Levobupivacaine.
Diphenhydramine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Diphenhydramine.
Benzocaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Benzocaine.
Chloroprocaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Chloroprocaine.
Phenol The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Phenol.
Tetrodotoxin The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Tetrodotoxin.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Benzyl alcohol.
Capsaicin The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Capsaicin.
Etidocaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Etidocaine.
Articaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Articaine.
Tetracaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Tetracaine.
Propoxycaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Propoxycaine.
Pramocaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Pramocaine.
Butamben The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Butamben.
Butacaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Butacaine.
Oxetacaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Oxetacaine.
Ethyl chloride The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Ethyl chloride.
Butanilicaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Butanilicaine.
Metabutethamine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Metabutethamine.
Quinisocaine The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Quinisocaine.
Cyclosporine The serum concentration of Elacestrant can be increased when it is combined with Cyclosporine.
Fluvoxamine The serum concentration of Elacestrant can be increased when it is combined with Fluvoxamine.
Fluconazole The serum concentration of Elacestrant can be increased when it is combined with Fluconazole.
Erythromycin The serum concentration of Elacestrant can be increased when it is combined with Erythromycin.
Ziprasidone The serum concentration of Elacestrant can be increased when it is combined with Ziprasidone.
Isradipine The serum concentration of Elacestrant can be increased when it is combined with Isradipine.
Diltiazem The serum concentration of Elacestrant can be increased when it is combined with Diltiazem.
Clozapine The serum concentration of Elacestrant can be increased when it is combined with Clozapine.
Haloperidol The serum concentration of Elacestrant can be increased when it is combined with Haloperidol.
Ciprofloxacin The serum concentration of Elacestrant can be increased when it is combined with Ciprofloxacin.
Voriconazole The serum concentration of Elacestrant can be increased when it is combined with Voriconazole.
Nicardipine The serum concentration of Elacestrant can be increased when it is combined with Nicardipine.
Verapamil The serum concentration of Elacestrant can be increased when it is combined with Verapamil.
Aprepitant The serum concentration of Elacestrant can be increased when it is combined with Aprepitant.
Isoniazid The serum concentration of Elacestrant can be increased when it is combined with Isoniazid.
Tioconazole The serum concentration of Elacestrant can be increased when it is combined with Tioconazole.
Primaquine The serum concentration of Elacestrant can be increased when it is combined with Primaquine.
Miconazole The serum concentration of Elacestrant can be increased when it is combined with Miconazole.
Danazol The serum concentration of Elacestrant can be increased when it is combined with Danazol.
Fusidic acid The serum concentration of Elacestrant can be increased when it is combined with Fusidic acid.
Zimelidine The serum concentration of Elacestrant can be increased when it is combined with Zimelidine.
Dronedarone The serum concentration of Elacestrant can be increased when it is combined with Dronedarone.
Milnacipran The serum concentration of Elacestrant can be increased when it is combined with Milnacipran.
Simeprevir The serum concentration of Elacestrant can be increased when it is combined with Simeprevir.
Isavuconazonium The serum concentration of Elacestrant can be increased when it is combined with Isavuconazonium.
Desvenlafaxine The serum concentration of Elacestrant can be increased when it is combined with Desvenlafaxine.
Nilvadipine The serum concentration of Elacestrant can be increased when it is combined with Nilvadipine.
Seproxetine The serum concentration of Elacestrant can be increased when it is combined with Seproxetine.
Crizotinib The serum concentration of Crizotinib can be increased when it is combined with Elacestrant.
Linagliptin The serum concentration of Elacestrant can be increased when it is combined with Linagliptin.
Luliconazole The serum concentration of Elacestrant can be increased when it is combined with Luliconazole.
Indalpine The serum concentration of Elacestrant can be increased when it is combined with Indalpine.
Netupitant The serum concentration of Elacestrant can be increased when it is combined with Netupitant.
Barnidipine The serum concentration of Elacestrant can be increased when it is combined with Barnidipine.
Benidipine The serum concentration of Elacestrant can be increased when it is combined with Benidipine.
Venetoclax The serum concentration of Elacestrant can be increased when it is combined with Venetoclax.
Isavuconazole The serum concentration of Elacestrant can be increased when it is combined with Isavuconazole.
Fosnetupitant The serum concentration of Elacestrant can be increased when it is combined with Fosnetupitant.
Berotralstat The serum concentration of Elacestrant can be increased when it is combined with Berotralstat.
Nelfinavir The serum concentration of Elacestrant can be increased when it is combined with Nelfinavir.
Indinavir The serum concentration of Elacestrant can be increased when it is combined with Indinavir.
Terfenadine The serum concentration of Elacestrant can be increased when it is combined with Terfenadine.
Ritonavir The serum concentration of Elacestrant can be increased when it is combined with Ritonavir.
Efavirenz The serum concentration of Elacestrant can be increased when it is combined with Efavirenz.
Ergotamine The serum concentration of Elacestrant can be increased when it is combined with Ergotamine.
Amprenavir The serum concentration of Elacestrant can be increased when it is combined with Amprenavir.
Delavirdine The serum concentration of Elacestrant can be increased when it is combined with Delavirdine.
Methimazole The serum concentration of Elacestrant can be increased when it is combined with Methimazole.
Conivaptan The serum concentration of Elacestrant can be increased when it is combined with Conivaptan.
Tipranavir The serum concentration of Elacestrant can be increased when it is combined with Tipranavir.
Telithromycin The serum concentration of Elacestrant can be increased when it is combined with Telithromycin.
Ketoconazole The serum concentration of Elacestrant can be increased when it is combined with Ketoconazole.
Atazanavir The serum concentration of Elacestrant can be increased when it is combined with Atazanavir.
Amiodarone The serum concentration of Elacestrant can be increased when it is combined with Amiodarone.
Econazole The serum concentration of Elacestrant can be increased when it is combined with Econazole.
Nefazodone The serum concentration of Elacestrant can be increased when it is combined with Nefazodone.
Itraconazole The serum concentration of Elacestrant can be increased when it is combined with Itraconazole.
Clarithromycin The serum concentration of Elacestrant can be increased when it is combined with Clarithromycin.
Saquinavir The serum concentration of Elacestrant can be increased when it is combined with Saquinavir.
Posaconazole The serum concentration of Elacestrant can be increased when it is combined with Posaconazole.
Darunavir The serum concentration of Elacestrant can be increased when it is combined with Darunavir.
Lopinavir The serum concentration of Elacestrant can be increased when it is combined with Lopinavir.
Ditiocarb The serum concentration of Elacestrant can be increased when it is combined with Ditiocarb.
Nilotinib The serum concentration of Elacestrant can be increased when it is combined with Nilotinib.

Target Protein

Estrogen receptor ESR1

Referensi & Sumber

Synthesis reference: Cruskie MP, et al. (2019). Polymorphic forms of RAD1901-2HCl (U.S. Patent No. 10,385,008 B2). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/42/82/b6/e9fcbbbd08054e/US10385008.pdf
Artikel (PubMed)
  • PMID: 35923930
    Lloyd MR, Wander SA, Hamilton E, Razavi P, Bardia A: Next-generation selective estrogen receptor degraders and other novel endocrine therapies for management of metastatic hormone receptor-positive breast cancer: current and emerging role. Ther Adv Med Oncol. 2022 Jul 30;14:17588359221113694. doi: 10.1177/17588359221113694. eCollection 2022.
  • PMID: 26164151
    Garner F, Shomali M, Paquin D, Lyttle CR, Hattersley G: RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models. Anticancer Drugs. 2015 Oct;26(9):948-56. doi: 10.1097/CAD.0000000000000271.
  • PMID: 28473534
    Bihani T, Patel HK, Arlt H, Tao N, Jiang H, Brown JL, Purandare DM, Hattersley G, Garner F: Elacestrant (RAD1901), a Selective Estrogen Receptor Degrader (SERD), Has Antitumor Activity in Multiple ER(+) Breast Cancer Patient-derived Xenograft Models. Clin Cancer Res. 2017 Aug 15;23(16):4793-4804. doi: 10.1158/1078-0432.CCR-16-2561. Epub 2017 May 4.
  • PMID: 31852484
    Patel HK, Tao N, Lee KM, Huerta M, Arlt H, Mullarkey T, Troy S, Arteaga CL, Bihani T: Elacestrant (RAD1901) exhibits anti-tumor activity in multiple ER+ breast cancer models resistant to CDK4/6 inhibitors. Breast Cancer Res. 2019 Dec 18;21(1):146. doi: 10.1186/s13058-019-1230-0.
  • PMID: 35584336
    Bidard FC, Kaklamani VG, Neven P, Streich G, Montero AJ, Forget F, Mouret-Reynier MA, Sohn JH, Taylor D, Harnden KK, Khong H, Kocsis J, Dalenc F, Dillon PM, Babu S, Waters S, Deleu I, Garcia Saenz JA, Bria E, Cazzaniga M, Lu J, Aftimos P, Cortes J, Liu S, Tonini G, Laurent D, Habboubi N, Conlan MG, Bardia A: Elacestrant (oral selective estrogen receptor degrader) Versus Standard Endocrine Therapy for Estrogen Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Advanced Breast Cancer: Results From the Randomized Phase III EMERALD Trial. J Clin Oncol. 2022 Oct 1;40(28):3246-3256. doi: 10.1200/JCO.22.00338. Epub 2022 May 18.
  • PMID: 31602686
    Chinnasamy K, Saravanan M, Poomani K: Investigation of binding mechanism and downregulation of elacestrant for wild and L536S mutant estrogen receptor-alpha through molecular dynamics simulation and binding free energy analysis. J Comput Chem. 2020 Jan 15;41(2):97-109. doi: 10.1002/jcc.26076. Epub 2019 Oct 10.
  • PMID: 33138369
    Lu Y, Liu W: Selective Estrogen Receptor Degraders (SERDs): A Promising Strategy for Estrogen Receptor Positive Endocrine-Resistant Breast Cancer. J Med Chem. 2020 Dec 24;63(24):15094-15114. doi: 10.1021/acs.jmedchem.0c00913. Epub 2020 Nov 2.

Contoh Produk & Brand

Produk: 4 • International brands: 1
Produk
  • Orserdu
    Tablet, film coated • 86 mg • Oral • EU • Approved
  • Orserdu
    Tablet, film coated • 345 mg • Oral • EU • Approved
  • Orserdu
    Tablet, film coated • 86 mg/1 • Oral • US • Approved
  • Orserdu
    Tablet, film coated • 345 mg/1 • Oral • US • Approved
International Brands
  • Orserdu — Stemline Therapeutics

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