Peringatan Keamanan

There are no data regarding overdosage with revumenib.

Revumenib

DB18515

small molecule approved investigational

Deskripsi

Abnormal gene rearrangements at chromosome locus 11q23, called KMT2A rearrangements or translocations, are present in 5%-10% of patients with acute leukemias and are the sole genetic aberration found in the majority of infant acute lymphoblastic leukemia cases.^A264688 Aberrant KMT2A is associated with the upregulation of leukemogenic transcription pathways, notably those involving HOXA genes and their co-factor MEIS1. Menin is a scaffold protein that interacts with both the wild-type and rearranged KMT2A, which is crucial for KMT2A activity and the maintenance of HOXA expression and leukemogenesis.^A264688

Revumenib is an oral small molecule menin inhibitor that prevents the interaction between menin and aberrant KMT2A. It was approved by the FDA in November 2024 for the treatment of leukemia with KMT2A aberrations,L51868,L51863 becoming the first menin inhibitor to receive FDA approval.^L51888

Struktur Molekul 2D

Berat 630.82

Wujud solid

Peta Jejaring Molekuler

Obat Target Gen Interaksi Enzim Transporter Carrier

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

1. Pendahuluan & Konsep

Fitur visualisasi ini dikembangkan menggunakan pendekatan Graph Theory untuk memetakan hubungan polifarmasi dan molekuler. Entitas (Obat, Target, Gen) direpresentasikan sebagai Simpul (Nodes), sedangkan hubungan biologisnya sebagai Sisi (Edges).

2. Sumber Data (Validasi)

Data Obat: Diekstraksi dari elemen drugbank-id dan name pada skema XML DrugBank.
Target Protein: Diambil dari elemen targets/target yang memuat polipeptida sasaran.
Genetik: Disinkronisasi dari sub-elemen gene-name dan varian snp-effects.
Genetik: Jumlah titik node dibatasi pada maksimal 10 (Slice=10) interaksi untuk menghindari tumpukan data.

3. Algoritma Visualisasi

Tata letak grafik menggunakan algoritma Force-Directed Graph (Barnes-Hut). Model fisika ini menerapkan gaya tolak-menolak antar simpul (Gravitasi: -3000) agar tidak tumpang tindih, serta gaya pegas (Spring: 0.04) pada garis penghubung untuk fleksibilitas interaksi.

4. Legenda Visual

Obat Utama (Pusat Analisis)

Target Protein (Mekanisme)

Gen (Faktor Genetik)

Metode ini mendukung analisis Precision Medicine dan evaluasi risiko Drug-Drug Interaction (DDI).

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following oral administration at a dose of 163 mg twice daily (and co-administered with strong CYP3A4 inhibitors), the half-life of revumenib was 7.5 hours.[L51863] At a dose of 276 mg (in patients without co-administered strong CYP3A4 inhibitors), the half-life of revumenib was 3.6 hours.[L51863]

Volume Distribusi The the geometric mean apparent volume of distribution of revumenib was 78 L.[L51863]

Klirens (Clearance) Following oral administration at a dose of 163 mg twice daily (and co-administered with strong CYP3A4 inhibitors), the apparent clearance of revumenib was 7 L/h.[L51863] At a dose of 276 mg (in patients without co-administered strong CYP3A4 inhibitors), the apparent clearance of revumenib was 27 L/h.[L51863]

Absorpsi

Following oral administration at a dose of 163 mg twice daily (and co-administered with strong CYP3A4 inhibitors), the C_max and AUC_0-12h were 3220 ng/mL and 22610 ng.h/mL, respectively, and the T_max was 2 hours.^L51863 At a dose of 276 mg (in patients without co-administered strong CYP3A4 inhibitors), the C_max and AUC_0-12h were 2052 ng/mL and 10150 ng.h/mL, respectively, and the T_max was 1 hour.^L51863

Metabolisme

Approximately 86% of an administered dose of revumenib is metabolized.^L51883 The enzyme primarily responsible for revumenib's metabolism is CYP3A4, while CYP2C8 and other unspecified liver enzymes appear to play a smaller role.L51863,L51883 The M1 metabolite, which is the primary circulating metabolite, is not active with respect to therapeutic efficacy but does contribute to revumenib's clinically significant effects on the QTc interval.^L51863 Other metabolites, including secondary metabolites, are known to exist but do not appear to be characterized in the literature.^L51883

Rute Eliminasi

Approximately 49% of administered revumenib is excreted in the feces (7% as unchanged parent drug) and 27% is excreted in the urine (7% as unchanged parent drug).^L51863

Interaksi Makanan

1 Data

1. Take on an empty stomach. Prescribing information for revumenib recommends administration on an empty stomach or with a small, low-fat meal.

Interaksi Obat

459 Data

Nelfinavir	The serum concentration of Revumenib can be increased when it is combined with Nelfinavir.
Indinavir	The serum concentration of Revumenib can be increased when it is combined with Indinavir.
Terfenadine	The serum concentration of Revumenib can be increased when it is combined with Terfenadine.
Ritonavir	The serum concentration of Revumenib can be increased when it is combined with Ritonavir.
Voriconazole	The serum concentration of Revumenib can be increased when it is combined with Voriconazole.
Efavirenz	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Efavirenz.
Ergotamine	The serum concentration of Revumenib can be increased when it is combined with Ergotamine.
Amprenavir	The serum concentration of Revumenib can be increased when it is combined with Amprenavir.
Delavirdine	The serum concentration of Revumenib can be increased when it is combined with Delavirdine.
Methimazole	The serum concentration of Revumenib can be increased when it is combined with Methimazole.
Conivaptan	The serum concentration of Revumenib can be increased when it is combined with Conivaptan.
Tipranavir	The serum concentration of Revumenib can be increased when it is combined with Tipranavir.
Telithromycin	The serum concentration of Revumenib can be increased when it is combined with Telithromycin.
Ketoconazole	The serum concentration of Revumenib can be increased when it is combined with Ketoconazole.
Atazanavir	The serum concentration of Revumenib can be increased when it is combined with Atazanavir.
Amiodarone	The serum concentration of Revumenib can be increased when it is combined with Amiodarone.
Econazole	The serum concentration of Revumenib can be increased when it is combined with Econazole.
Nefazodone	The serum concentration of Revumenib can be increased when it is combined with Nefazodone.
Itraconazole	The serum concentration of Revumenib can be increased when it is combined with Itraconazole.
Clarithromycin	The serum concentration of Revumenib can be increased when it is combined with Clarithromycin.
Saquinavir	The serum concentration of Revumenib can be increased when it is combined with Saquinavir.
Posaconazole	The serum concentration of Revumenib can be increased when it is combined with Posaconazole.
Darunavir	The serum concentration of Revumenib can be increased when it is combined with Darunavir.
Danazol	The serum concentration of Revumenib can be increased when it is combined with Danazol.
Lopinavir	The serum concentration of Revumenib can be increased when it is combined with Lopinavir.
Ditiocarb	The serum concentration of Revumenib can be increased when it is combined with Ditiocarb.
Nilotinib	The serum concentration of Revumenib can be increased when it is combined with Nilotinib.
Telaprevir	The serum concentration of Revumenib can be increased when it is combined with Telaprevir.
Levoketoconazole	The serum concentration of Revumenib can be increased when it is combined with Levoketoconazole.
Lonafarnib	The serum concentration of Revumenib can be increased when it is combined with Lonafarnib.
Midostaurin	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Midostaurin.
Boceprevir	The serum concentration of Revumenib can be increased when it is combined with Boceprevir.
Elvitegravir	The serum concentration of Revumenib can be increased when it is combined with Elvitegravir.
Stiripentol	The serum concentration of Revumenib can be increased when it is combined with Stiripentol.
Curcumin	The serum concentration of Revumenib can be increased when it is combined with Curcumin.
Ribociclib	The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Revumenib.
Danoprevir	The serum concentration of Revumenib can be increased when it is combined with Danoprevir.
Troleandomycin	The serum concentration of Revumenib can be increased when it is combined with Troleandomycin.
Phenytoin	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Phenytoin.
Pentobarbital	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Pentobarbital.
Carbamazepine	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Carbamazepine.
Mitotane	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Mitotane.
Primidone	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Primidone.
Rimexolone	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Rimexolone.
Rifampin	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Rifampin.
Phenobarbital	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Phenobarbital.
Rifapentine	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Rifapentine.
Dexamethasone	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Dexamethasone.
Fosphenytoin	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Fosphenytoin.
St. John's Wort	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with St. John's Wort.
Enzalutamide	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Enzalutamide.
Lumacaftor	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Lumacaftor.
Apalutamide	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Apalutamide.
Bexarotene	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Bexarotene.
Bosentan	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Bosentan.
Nafcillin	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Nafcillin.
Modafinil	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Modafinil.
Etravirine	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Etravirine.
Avasimibe	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Avasimibe.
Echinacea	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Echinacea.
Dexamethasone acetate	The serum concentration of M1 metabolite, an active metabolite of Revumenib, can be increased when used in combination with Dexamethasone acetate.
Leuprolide	The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Revumenib.
Goserelin	The risk or severity of QTc prolongation can be increased when Goserelin is combined with Revumenib.
Octreotide	The risk or severity of QTc prolongation can be increased when Octreotide is combined with Revumenib.
Oxytocin	The risk or severity of QTc prolongation can be increased when Oxytocin is combined with Revumenib.
Esmolol	The risk or severity of QTc prolongation can be increased when Esmolol is combined with Revumenib.
Bortezomib	The risk or severity of QTc prolongation can be increased when Bortezomib is combined with Revumenib.
Betaxolol	The risk or severity of QTc prolongation can be increased when Betaxolol is combined with Revumenib.
Fluconazole	The risk or severity of QTc prolongation can be increased when Fluconazole is combined with Revumenib.
Erythromycin	The serum concentration of Revumenib can be increased when it is combined with Erythromycin.
Dofetilide	The risk or severity of QTc prolongation can be increased when Dofetilide is combined with Revumenib.
Azithromycin	The risk or severity of QTc prolongation can be increased when Azithromycin is combined with Revumenib.
Citalopram	The risk or severity of QTc prolongation can be increased when Revumenib is combined with Citalopram.
Moxifloxacin	The risk or severity of QTc prolongation can be increased when Moxifloxacin is combined with Revumenib.
Pregabalin	The risk or severity of QTc prolongation can be increased when Pregabalin is combined with Revumenib.
Ranolazine	The risk or severity of QTc prolongation can be increased when Ranolazine is combined with Revumenib.
Benzatropine	The risk or severity of QTc prolongation can be increased when Benzatropine is combined with Revumenib.
Ziprasidone	The risk or severity of QTc prolongation can be increased when Revumenib is combined with Ziprasidone.
Anagrelide	The risk or severity of QTc prolongation can be increased when Anagrelide is combined with Revumenib.
Sulfisoxazole	The risk or severity of QTc prolongation can be increased when Sulfisoxazole is combined with Revumenib.
Isradipine	The risk or severity of QTc prolongation can be increased when Isradipine is combined with Revumenib.
Disopyramide	The risk or severity of QTc prolongation can be increased when Disopyramide is combined with Revumenib.
Clemastine	The risk or severity of QTc prolongation can be increased when Clemastine is combined with Revumenib.
Atomoxetine	The risk or severity of QTc prolongation can be increased when Atomoxetine is combined with Revumenib.
Ibutilide	The risk or severity of QTc prolongation can be increased when Ibutilide is combined with Revumenib.
Valproic acid	The risk or severity of QTc prolongation can be increased when Valproic acid is combined with Revumenib.
Amitriptyline	The risk or severity of QTc prolongation can be increased when Amitriptyline is combined with Revumenib.
Methadone	The risk or severity of QTc prolongation can be increased when Methadone is combined with Revumenib.
Olanzapine	The risk or severity of QTc prolongation can be increased when Olanzapine is combined with Revumenib.
Cetirizine	The risk or severity of QTc prolongation can be increased when Cetirizine is combined with Revumenib.
Diltiazem	The risk or severity of QTc prolongation can be increased when Diltiazem is combined with Revumenib.
Protriptyline	The risk or severity of QTc prolongation can be increased when Protriptyline is combined with Revumenib.
Alfuzosin	The risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Revumenib.
Trimethadione	The risk or severity of QTc prolongation can be increased when Trimethadione is combined with Revumenib.
Buclizine	The risk or severity of QTc prolongation can be increased when Buclizine is combined with Revumenib.
Mefloquine	The risk or severity of QTc prolongation can be increased when Mefloquine is combined with Revumenib.
Clozapine	The risk or severity of QTc prolongation can be increased when Revumenib is combined with Clozapine.
Grepafloxacin	The risk or severity of QTc prolongation can be increased when Grepafloxacin is combined with Revumenib.
Doxylamine	The risk or severity of QTc prolongation can be increased when Doxylamine is combined with Revumenib.
Mirtazapine	The risk or severity of QTc prolongation can be increased when Mirtazapine is combined with Revumenib.

Target Protein

Menin MEN1

Referensi & Sumber

Artikel (PubMed)

PMID: 39086307
Salman MY, Stein EM: Revumenib for patients with acute leukemia: a new tool for differentiation therapy. Haematologica. 2024 Nov 1;109(11):3488-3495. doi: 10.3324/haematol.2022.282621.

Link

Contoh Produk & Brand

Produk: 3 • International brands: 0

Produk

Revuforj

Tablet, film coated • 25 mg/1 • Oral • US • Approved
Revuforj

Tablet, film coated • 110 mg/1 • Oral • US • Approved
Revuforj

Tablet, film coated • 160 mg/1 • Oral • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.