New primary malignancies, cutaneous and non-cutaneous, have been observed in patients treated with BRAF inhibitors and can occur with encorafenib.L12216
In COLUMBUS, a phase 3 safety and efficacy trial,L12216 cutaneous squamous cell carcinoma (cuSCC), including keratoacanthoma (KA), occurred in 2.6%, and basal cell carcinoma occurred in 1.6% of patients who received BRAFTOVI in combination with binimetinib. The median time to first occurrence of cuSCC/KA was 5.8 months (range 1 to 9 months).L12216
Tumor promotion in BRAF Wild-Type Tumors has been observed with encofarenib use.L12216
Hemorrhage, uveitis, QT interval prolongation are also other adverse events observed while taking this medication.L12216
Encorafenib, when used as a single agent, is associated with an increased risk of certain adverse reactions compared to when BRAFTOVI is used in combination with binimetinib. Grades 3 or 4 dermatologic reactions occurred in 21% of patients treated with BRAFTOVI therapy alone compared to 2% of patients treated with BRAFTOVI in combination with binimetinib.L12216
Advise females with reproductive potential of the potential risk to a fetus. Advise females of reproductive potential to use effective non-hormonal contraception during treatment with BRAFTOVI and for 2 weeks after the final dose.L12216
Carcinogenicity studies with encorafenib have not been conducted. Encorafenib was not genotoxic in studies evaluating reverse mutations in bacteria, chromosomal aberrations in mammalian cells, or micronuclei in the bone marrow of rats.L48581
No dedicated fertility studies were performed with encorafenib in animals. In a general toxicology study in rats, decreased testes and epididymis weights, tubular degeneration in testes, and oligospermia in epididymides were observed at doses approximately 13 times the human exposure at the 450 mg clinical dose based on AUC. No effects on reproductive organs were observed in either sex in any of the non-human primate toxicity studies.L48581
Since encorafenib is 86% bound to plasma proteins, hemodialysis is likely to be ineffective in the treatment of overdose with encorafenib.L48581
Encorafenib, also known as BRAFTOVI, is a kinase inhibitor. Encorafenib inhibits BRAF gene, which encodes for B-raf protein, which is a proto-oncogene involved in various genetic mutations.L12216 This protein plays a role in regulating the MAP kinase/ERK signaling pathway, which impacts cell division, differentiation, and secretion. Mutations in this gene, most frequently the V600E mutation, are the most commonly identified cancer-causing mutations in melanoma, and have been isolated in various other cancers as well, including non-Hodgkin lymphoma, colorectal cancer, thyroid carcinoma, non-small cell lung carcinoma, hairy cell leukemia and adenocarcinoma of the lung.L3344
On June 27, 2018, the Food and Drug Administration approved encorafenib and binimetinib (BRAFTOVI and MEKTOVI, Array BioPharma Inc.) in combination for patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test.L12216
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).
drugbank-id dan name pada skema XML DrugBank.targets/target yang memuat polipeptida sasaran.gene-name dan varian snp-effects.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.
| Ivabradine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Ivabradine. |
| Mirabegron | The serum concentration of Encorafenib can be increased when it is combined with Mirabegron. |
| Dofetilide | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Dofetilide. |
| Anagrelide | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Anagrelide. |
| Disopyramide | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Disopyramide. |
| Ibutilide | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Ibutilide. |
| Grepafloxacin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Grepafloxacin. |
| Toremifene | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Toremifene. |
| Trovafloxacin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Trovafloxacin. |
| Arsenic trioxide | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Arsenic trioxide. |
| Sparfloxacin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Sparfloxacin. |
| Lithium cation | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Lithium cation. |
| Temafloxacin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Temafloxacin. |
| Vandetanib | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Vandetanib. |
| Romidepsin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Romidepsin. |
| Asenapine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Asenapine. |
| Artemether | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Artemether. |
| Glasdegib | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Glasdegib. |
| Macimorelin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Macimorelin. |
| Terodiline | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Terodiline. |
| Citalopram | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Citalopram. |
| Clemastine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Clemastine. |
| Mifepristone | The serum concentration of Mifepristone can be decreased when it is combined with Encorafenib. |
| Cocaine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Cocaine. |
| Bepridil | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Bepridil. |
| Eliglustat | The metabolism of Eliglustat can be decreased when combined with Encorafenib. |
| Imatinib | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Imatinib. |
| Vemurafenib | The serum concentration of Encorafenib can be increased when it is combined with Vemurafenib. |
| Domperidone | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Domperidone. |
| Paliperidone | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Paliperidone. |
| Zuclopenthixol | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Zuclopenthixol. |
| Tetrabenazine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Tetrabenazine. |
| Iloperidone | The metabolism of Iloperidone can be decreased when combined with Encorafenib. |
| Deutetrabenazine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Deutetrabenazine. |
| Valproic acid | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Valproic acid. |
| Leuprolide | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Leuprolide. |
| Goserelin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Goserelin. |
| Moxifloxacin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Moxifloxacin. |
| Sulfisoxazole | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Sulfisoxazole. |
| Sulpiride | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Sulpiride. |
| Nimodipine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Nimodipine. |
| Droperidol | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Droperidol. |
| Oxaliplatin | The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Encorafenib. |
| Fluorouracil | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Fluorouracil. |
| Perflutren | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Perflutren. |
| Atropine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Atropine. |
| Adenosine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Adenosine. |
| Gadobenic acid | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Gadobenic acid. |
| Carbinoxamine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Carbinoxamine. |
| Nalidixic acid | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Nalidixic acid. |
| Cinoxacin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Cinoxacin. |
| Granisetron | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Granisetron. |
| Levosimendan | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Levosimendan. |
| Desloratadine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Desloratadine. |
| Lomefloxacin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Lomefloxacin. |
| Dimenhydrinate | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Dimenhydrinate. |
| Papaverine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Papaverine. |
| Levofloxacin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Levofloxacin. |
| Gemifloxacin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Gemifloxacin. |
| Ofloxacin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Ofloxacin. |
| Levacetylmethadol | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Levacetylmethadol. |
| Probucol | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Probucol. |
| Aceprometazine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Aceprometazine. |
| Terlipressin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Terlipressin. |
| Prenylamine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Prenylamine. |
| Fluspirilene | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Fluspirilene. |
| Azimilide | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Azimilide. |
| Pracinostat | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Pracinostat. |
| Technetium Tc-99m ciprofloxacin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Technetium Tc-99m ciprofloxacin. |
| Garenoxacin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Garenoxacin. |
| Tedisamil | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Tedisamil. |
| Tucidinostat | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Tucidinostat. |
| Telavancin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Telavancin. |
| Nemonoxacin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Nemonoxacin. |
| Antazoline | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Antazoline. |
| Bedaquiline | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Bedaquiline. |
| Fendiline | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Fendiline. |
| Eperisone | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Eperisone. |
| Butriptyline | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Butriptyline. |
| Amifampridine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Amifampridine. |
| Mocetinostat | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Mocetinostat. |
| Entinostat | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Entinostat. |
| CUDC-101 | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with CUDC-101. |
| Simendan | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Simendan. |
| Ricolinostat | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Ricolinostat. |
| Abexinostat | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Abexinostat. |
| Oxatomide | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Oxatomide. |
| Sitafloxacin | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Sitafloxacin. |
| Sultopride | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Sultopride. |
| Otilonium | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Otilonium. |
| Nizofenone | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Nizofenone. |
| Bunaftine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Bunaftine. |
| Lorcainide | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Lorcainide. |
| Penfluridol | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Penfluridol. |
| Dexverapamil | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Dexverapamil. |
| Emedastine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Emedastine. |
| Pazopanib | The serum concentration of Pazopanib can be increased when it is combined with Encorafenib. |
| Diltiazem | The serum concentration of Encorafenib can be increased when it is combined with Diltiazem. |
| Promazine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Promazine. |
| Prochlorperazine | The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Prochlorperazine. |