trametinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
MEK (MAPK kinase) tyrosine kinase inhibitors	4802	871700-17-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: GSK1120212B trametinib dimethyl sulfoxide trametinib GSK1120212 mekinist	a reversible inhibitor of mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and MEK2 activation and of MEK1 and MEK2 kinase activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway, which promotes cellular proliferation Molecular weight: 615.40 Formula: C26H23FIN5O4 CLOGP: 4.68 LIPINSKI: 1 HAC: 9 HDO: 2 TPSA: 102.06 ALOGS: -4.30 ROTB: 5 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

GSK1120212B
trametinib dimethyl sulfoxide
trametinib
GSK1120212
mekinist

a reversible inhibitor of mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and MEK2 activation and of MEK1 and MEK2 kinase activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway, which promotes cellular proliferation

Molecular weight: 615.40
Formula: C26H23FIN5O4
CLOGP: 4.68
LIPINSKI: 1
HAC: 9
HDO: 2
TPSA: 102.06
ALOGS: -4.30
ROTB: 5

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
2	mg	O

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	13.94 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.03 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	229 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company
May 29, 2013	FDA	NOVARTIS PHARMS CORP
March 28, 2016	PMDA	Novartis Pharma K.K.
June 30, 2014	EMA	NOVARTIS EUROPHARM LIMITED

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Pyrexia	1326.38	18.99	1053	16096	469425	63002448
Malignant neoplasm progression	1021.03	18.99	479	16670	81642	63390231
Chills	372.09	18.99	280	16869	113098	63358775
Product use in unapproved indication	335.15	18.99	320	16829	178760	63293113
Death	299.65	18.99	432	16717	373949	63097924
Uveitis	225.26	18.99	95	17054	12458	63459415
Visual impairment	196.93	18.99	171	16978	84275	63387598
Metastases to central nervous system	188.91	18.99	85	17064	13020	63458853
Rash	183.09	18.99	440	16709	560431	62911442
Ejection fraction decreased	135.58	18.99	81	17068	22251	63449622
Dermatitis acneiform	124.85	18.99	48	17101	4948	63466925
Panniculitis	124.41	18.99	61	17088	11324	63460549
Blood creatine phosphokinase increased	112.70	18.99	81	17068	30349	63441524
Skin toxicity	92.36	18.99	38	17111	4676	63467197
Drug ineffective	84.81	18.99	95	17054	1044670	62427203
Vision blurred	77.28	18.99	109	17040	91815	63380058
Erythema nodosum	71.44	18.99	32	17117	4843	63467030
Paronychia	70.47	18.99	33	17116	5532	63466341
Serous retinal detachment	65.45	18.99	16	17133	351	63471522
Chorioretinopathy	65.39	18.99	19	17130	820	63471053
Dry skin	56.22	18.99	73	17076	56814	63415059
Acne	53.85	18.99	47	17102	23246	63448627
Metastatic malignant melanoma	53.02	18.99	18	17131	1297	63470576
Drug hypersensitivity	52.81	18.99	10	17139	310677	63161196
Condition aggravated	51.73	18.99	22	17127	402195	63069678
Vogt-Koyanagi-Harada disease	50.12	18.99	11	17138	147	63471726
Haemophagocytic lymphohistiocytosis	45.66	18.99	31	17118	10596	63461277
Aspartate aminotransferase increased	45.63	18.99	85	17064	90192	63381681
Nausea	45.61	18.99	389	16760	854082	62617791
Lipase increased	45.22	18.99	30	17119	9870	63462003
BRAF V600E mutation positive	44.87	18.99	8	17141	32	63471841
Detachment of retinal pigment epithelium	44.75	18.99	12	17137	384	63471489
Hyperpyrexia	44.33	18.99	21	17128	3611	63468262
Second primary malignancy	43.51	18.99	27	17122	7926	63463947
Diarrhoea	43.16	18.99	335	16814	715031	62756842
Metastases to lung	42.80	18.99	32	17117	12718	63459155
Blood lactate dehydrogenase increased	42.44	18.99	41	17108	23075	63448798
Sinusitis	41.37	18.99	6	17143	226647	63245226
Metastasis	39.96	18.99	22	17127	5175	63466698
Erythema multiforme	39.78	18.99	28	17121	10141	63461732
Arthropathy	38.95	18.99	8	17141	234784	63237089
Vomiting	38.79	18.99	271	16878	559346	62912527
Rash maculo-papular	38.04	18.99	45	17104	31851	63440022
Dehydration	37.11	18.99	117	17032	173237	63298636
Glossodynia	37.04	18.99	3	17146	178873	63293000
Metastases to meninges	34.71	18.99	16	17133	2586	63469287
Fall	34.63	18.99	33	17116	392301	63079572
Wound	33.09	18.99	3	17146	163260	63308613
Pneumonitis	32.93	18.99	44	17105	35178	63436695
Non-small cell lung cancer recurrent	32.22	18.99	7	17142	89	63471784
Iridocyclitis	32.07	18.99	15	17134	2507	63469366
Discomfort	31.56	18.99	4	17145	167370	63304503
Rhabdomyolysis	30.97	18.99	48	17101	43903	63427970
Abdominal discomfort	30.70	18.99	25	17124	320860	63151013
Systemic inflammatory response syndrome	30.54	18.99	19	17130	5602	63466271
Malignant melanoma	30.53	18.99	25	17124	11331	63460542
Alanine aminotransferase increased	29.93	18.99	78	17071	103692	63368181
Vitreous floaters	29.50	18.99	19	17130	5947	63465926
Retinal detachment	29.49	18.99	19	17130	5950	63465923
Erysipelas	29.15	18.99	21	17128	7884	63463989
Melanoma recurrent	28.79	18.99	7	17142	150	63471723
Metastases to peritoneum	27.65	18.99	15	17134	3427	63468446
Joint swelling	27.25	18.99	29	17120	327637	63144236
Musculoskeletal stiffness	25.51	18.99	9	17140	184609	63287264
Disease progression	25.47	18.99	82	17067	122676	63349197
Serous retinopathy	25.45	18.99	5	17144	37	63471836
Weight increased	25.34	18.99	20	17129	260772	63211101
Panniculitis lobular	25.22	18.99	5	17144	39	63471834
Chest pain	24.41	18.99	14	17135	215945	63255928
Metastases to liver	24.38	18.99	31	17118	23608	63448265
Hypersensitivity	24.23	18.99	26	17123	292659	63179214
Sepsis	23.80	18.99	93	17056	153030	63318843
Metastases to spleen	23.43	18.99	6	17143	160	63471713
Immune-mediated hepatitis	23.33	18.99	10	17139	1361	63470512
Swelling	23.31	18.99	24	17125	275354	63196519
Insomnia	22.87	18.99	15	17134	215237	63256636
Metastases to lymph nodes	22.02	18.99	18	17131	8140	63463733
Leukoderma	21.77	18.99	5	17144	83	63471790
Nasopharyngitis	21.70	18.99	22	17127	254235	63217638
C-reactive protein increased	21.24	18.99	65	17084	94642	63377231
Sarcoid-like reaction	20.95	18.99	4	17145	25	63471848
Pancreatitis	20.90	18.99	43	17106	49012	63422861
Hepatitis	20.76	18.99	38	17111	39750	63432123
Acute polyneuropathy	20.65	18.99	6	17143	259	63471614
Drug interaction	20.51	18.99	19	17130	229112	63242761
Infective glossitis	19.67	18.99	4	17145	36	63471837
Treatment failure	19.66	18.99	15	17134	199028	63272845
Metastatic neoplasm	19.58	18.99	13	17136	4282	63467591
Decreased appetite	19.36	18.99	125	17024	250927	63220946
Transaminases increased	19.01	18.99	32	17117	31335	63440538

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Pyrexia	1272.24	17.89	1149	16212	331864	34607706
Malignant neoplasm progression	820.29	17.89	521	16840	87525	34852045
Metastases to central nervous system	395.56	17.89	150	17211	8055	34931515
Chills	379.70	17.89	317	17044	80726	34858844
Death	251.77	17.89	585	16776	397464	34542106
Product use in unapproved indication	195.59	17.89	265	17096	117234	34822336
Ejection fraction decreased	186.46	17.89	117	17244	19037	34920533
Rash	132.87	17.89	321	17040	222431	34717139
Visual impairment	121.50	17.89	117	17244	35685	34903885
Uveitis	118.72	17.89	63	17298	7472	34932098
Blood creatine phosphokinase increased	109.73	17.89	123	17238	44734	34894836
Metastases to liver	86.50	17.89	64	17297	13599	34925971
Dermatitis acneiform	81.59	17.89	46	17315	6143	34933427
Second primary malignancy	73.76	17.89	47	17314	7839	34931731
Metastases to stomach	71.64	17.89	15	17346	79	34939491
Metastases to lung	68.95	17.89	48	17313	9272	34930298
Melanoma recurrent	64.46	17.89	15	17346	137	34939433
Acne	63.75	17.89	49	17312	11017	34928553
Chorioretinopathy	63.71	17.89	25	17336	1468	34938102
Drug interaction	59.72	17.89	19	17342	225927	34713643
Hyperpyrexia	54.60	17.89	27	17334	2761	34936809
Malignant melanoma	53.69	17.89	39	17322	8051	34931519
Metastatic malignant melanoma	52.82	17.89	24	17337	2031	34937539
Blood lactate dehydrogenase increased	51.04	17.89	60	17301	22930	34916640
Haemophagocytic lymphohistiocytosis	48.95	17.89	45	17316	12928	34926642
Vision blurred	48.38	17.89	84	17277	45879	34893691
C-reactive protein increased	47.00	17.89	91	17270	54007	34885563
Paronychia	44.05	17.89	25	17336	3380	34936190
Serous retinal detachment	43.80	17.89	15	17346	597	34938973
Metastases to lymph nodes	43.77	17.89	28	17333	4700	34934870
Fatigue	41.00	17.89	319	17042	370334	34569236
Metastases to meninges	40.62	17.89	18	17343	1436	34938134
Toxicity to various agents	40.13	17.89	25	17336	200337	34739233
Metastases to peritoneum	39.54	17.89	19	17342	1825	34937745
Metastases to bone	38.47	17.89	38	17323	11932	34927638
Detachment of retinal pigment epithelium	38.21	17.89	13	17348	507	34939063
Malignant mesenteric neoplasm	37.91	17.89	8	17353	44	34939526
Metastases to skin	35.98	17.89	12	17349	440	34939130
Off label use	35.29	17.89	100	17261	419424	34520146
Drug ineffective	34.77	17.89	114	17247	456637	34482933
Procalcitonin increased	34.42	17.89	17	17344	1734	34937836
Skin toxicity	33.89	17.89	24	17337	4760	34934810
Jejunal ulcer perforation	33.20	17.89	8	17353	86	34939484
Panniculitis	32.33	17.89	17	17344	1977	34937593
Metastasis	32.19	17.89	22	17339	4122	34935448
Squamous cell carcinoma	30.68	17.89	33	17328	11442	34928128
Decreased appetite	29.87	17.89	162	17199	166230	34773340
Intestinal metastasis	29.47	17.89	9	17352	247	34939323
Metastases to heart	29.23	17.89	8	17353	147	34939423
Omental necrosis	28.91	17.89	6	17355	30	34939540
Anxiety	28.76	17.89	7	17354	99421	34840149
Condition aggravated	28.60	17.89	32	17329	192164	34747406
Mesenteric neoplasm	28.59	17.89	6	17355	32	34939538
Tissue infiltration	28.58	17.89	7	17354	81	34939489
Vomiting	28.33	17.89	215	17146	247406	34692164
Gastrointestinal wall thickening	27.84	17.89	14	17347	1484	34938086
Basal cell carcinoma	27.63	17.89	41	17320	19617	34919953
Ureteral disorder	27.62	17.89	8	17353	182	34939388
Eastern Cooperative Oncology Group performance status	27.58	17.89	6	17355	39	34939531
Overdose	27.15	17.89	6	17355	91053	34848517
Retinal detachment	27.03	17.89	22	17339	5369	34934201
Dehydration	26.40	17.89	131	17230	129838	34809732
Brain neoplasm	24.84	17.89	17	17344	3192	34936378
Nausea	24.04	17.89	266	17095	339642	34599928
Dry skin	24.01	17.89	50	17311	31237	34908333
Influenza like illness	23.39	17.89	46	17315	27588	34911982
Erythema nodosum	22.93	17.89	12	17349	1382	34938188
Depression	22.53	17.89	10	17351	97088	34842482
Papilloedema	22.50	17.89	15	17346	2698	34936872
Febrile neutropenia	22.37	17.89	21	17340	136828	34802742
Abdominal lymphadenopathy	22.03	17.89	10	17351	844	34938726
Left ventricular dysfunction	22.01	17.89	26	17335	9981	34929589
Concomitant disease aggravated	21.94	17.89	20	17341	5681	34933889
Myocardial infarction	21.71	17.89	17	17344	121068	34818502
Dermatitis	21.49	17.89	25	17336	9443	34930127
General physical health deterioration	21.08	17.89	122	17239	128147	34811423
BRAF gene mutation	20.64	17.89	5	17356	55	34939515
Metastases to adrenals	20.41	17.89	10	17351	1002	34938568
Fat necrosis	20.08	17.89	7	17354	294	34939276
Liver function test increased	19.92	17.89	30	17331	14535	34925035
Tumour invasion	19.83	17.89	7	17354	305	34939265
Blood alkaline phosphatase increased	19.60	17.89	46	17315	31129	34908441
Therapy partial responder	19.54	17.89	24	17337	9592	34929978
Cerebral haemorrhage	19.25	17.89	49	17312	34888	34904682
Leukoderma	19.03	17.89	5	17356	78	34939492
Blood pressure increased	19.03	17.89	10	17351	88092	34851478
Brain neoplasm malignant	18.92	17.89	9	17352	845	34938725
Retinopathy	18.55	17.89	12	17349	2052	34937518
Iridocyclitis	18.38	17.89	11	17350	1641	34937929
Small intestine carcinoma	18.15	17.89	8	17353	630	34938940
Pneumonitis	18.13	17.89	47	17314	33831	34905739
General physical condition abnormal	17.99	17.89	15	17346	3784	34935786

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Pyrexia	1929.60	16.52	1694	25864	677015	79039815
Malignant neoplasm progression	1456.73	16.52	776	26782	135214	79581616
Chills	478.62	16.52	415	27143	159819	79557011
Metastases to central nervous system	438.59	16.52	177	27381	16198	79700632
Death	361.73	16.52	676	26882	565838	79150992
Ejection fraction decreased	326.13	16.52	182	27376	34395	79682435
Uveitis	273.79	16.52	128	27430	16702	79700128
Product use in unapproved indication	225.53	16.52	349	27209	250010	79466820
Blood creatine phosphokinase increased	208.71	16.52	177	27381	65913	79650917
Dermatitis acneiform	181.29	16.52	82	27476	9911	79706919
Rash	145.41	16.52	484	27074	577874	79138956
Chorioretinopathy	126.71	16.52	42	27516	2189	79714641
Panniculitis	110.83	16.52	63	27495	12308	79704522
Paronychia	104.59	16.52	52	27506	7756	79709074
Blood lactate dehydrogenase increased	101.82	16.52	94	27464	39076	79677754
Serous retinal detachment	98.87	16.52	29	27529	1005	79715825
Metastases to lung	97.99	16.52	67	27491	18096	79698734
Second primary malignancy	97.11	16.52	61	27497	14289	79702541
Haemophagocytic lymphohistiocytosis	95.77	16.52	71	27487	21766	79695064
Metastases to liver	93.79	16.52	78	27480	28236	79688594
Hyperpyrexia	88.86	16.52	43	27515	6049	79710781
Detachment of retinal pigment epithelium	87.41	16.52	25	27533	791	79716039
Drug ineffective	85.77	16.52	152	27406	1080761	78636069
Skin toxicity	84.48	16.52	46	27512	8268	79708562
Melanoma recurrent	81.97	16.52	19	27539	253	79716577
Erythema nodosum	75.95	16.52	37	27521	5280	79711550
Visual impairment	73.87	16.52	122	27436	92009	79624821
Condition aggravated	73.43	16.52	41	27517	501083	79215747
Metastatic malignant melanoma	73.36	16.52	30	27528	2833	79713997
C-reactive protein increased	69.58	16.52	144	27414	128883	79587947
Malignant melanoma	69.33	16.52	50	27508	14691	79702139
Metastasis	66.96	16.52	37	27521	6843	79709987
Drug hypersensitivity	65.62	16.52	12	27546	298904	79417926
Metastases to lymph nodes	64.89	16.52	42	27516	10355	79706475
Metastases to peritoneum	64.19	16.52	31	27527	4341	79712489
Drug interaction	63.69	16.52	32	27526	415151	79301679
Metastases to stomach	60.13	16.52	15	27543	277	79716553
Aspartate aminotransferase increased	59.27	16.52	141	27417	138500	79578330
Dehydration	58.78	16.52	204	27354	247983	79468847
Procalcitonin increased	58.77	16.52	26	27532	2980	79713850
Squamous cell carcinoma	57.98	16.52	46	27512	15576	79701254
Metastases to meninges	57.34	16.52	27	27531	3574	79713256
Rheumatoid arthritis	56.56	16.52	4	27554	208466	79508364
Lipase increased	55.85	16.52	46	27512	16420	79700410
Retinal detachment	54.40	16.52	36	27522	9211	79707619
Toxicity to various agents	52.90	16.52	41	27517	421499	79295331
BRAF V600E mutation positive	52.86	16.52	10	27548	44	79716786
Rash maculo-papular	51.46	16.52	79	27479	55999	79660831
Iridocyclitis	50.59	16.52	25	27533	3679	79713151
Metastases to bone	49.21	16.52	51	27507	24376	79692454
Vogt-Koyanagi-Harada disease	47.34	16.52	12	27546	237	79716593
Vomiting	46.88	16.52	391	27167	665437	79051393
Vision blurred	45.57	16.52	108	27450	105790	79611040
Dry skin	45.30	16.52	83	27475	67912	79648918
Sinusitis	44.76	16.52	7	27551	195494	79521336
Metastases to skin	43.80	16.52	18	27540	1721	79715109
Pneumonitis	42.72	16.52	76	27482	60784	79656046
Decreased appetite	42.08	16.52	231	27327	342187	79374643
Malignant mesenteric neoplasm	39.53	16.52	8	27550	53	79716777
BRAF gene mutation	38.79	16.52	8	27550	59	79716771
Alanine aminotransferase increased	37.90	16.52	133	27425	162437	79554393
Blood alkaline phosphatase increased	37.81	16.52	74	27484	63590	79653240
Off label use	37.42	16.52	174	27384	907041	78809789
Overdose	37.11	16.52	9	27549	184197	79532633
Therapy partial responder	36.26	16.52	37	27521	17360	79699470
Anxiety	35.38	16.52	21	27537	248491	79468339
Joint swelling	35.02	16.52	29	27529	288617	79428213
Therapeutic product effect incomplete	34.97	16.52	4	27554	141641	79575189
Metastases to adrenals	34.29	16.52	14	27544	1316	79715514
Abdominal lymphadenopathy	34.25	16.52	14	27544	1320	79715510
Jejunal ulcer perforation	33.44	16.52	8	27550	123	79716707
Basal cell carcinoma	33.37	16.52	52	27506	37323	79679507
Intestinal metastasis	33.31	16.52	10	27548	376	79716454
Product dose omission issue	32.40	16.52	23	27535	247514	79469316
Arthropathy	31.37	16.52	11	27547	177100	79539730
Weight increased	31.09	16.52	30	27528	277356	79439474
Musculoskeletal stiffness	30.78	16.52	11	27547	174997	79541833
Fall	30.58	16.52	78	27480	487551	79229279
Nasopharyngitis	30.18	16.52	26	27532	253855	79462975
Dermatitis	30.09	16.52	37	27521	21284	79695546
Insomnia	29.28	16.52	25	27533	245145	79471685
Visual acuity reduced	29.14	16.52	43	27515	29426	79687404
Omental necrosis	29	16.52	6	27552	45	79716785
Blood pressure increased	28.51	16.52	19	27539	211341	79505489
Non-small cell lung cancer recurrent	28.49	16.52	7	27551	121	79716709
Eastern Cooperative Oncology Group performance status	28.44	16.52	6	27552	50	79716780
Erysipelas	28.11	16.52	26	27532	10824	79706006
Demyelinating polyneuropathy	27.66	16.52	13	27545	1713	79715117
Retinopathy	27.48	16.52	17	27541	3874	79712956
Concomitant disease aggravated	27.44	16.52	28	27530	13139	79703691
Acne	27.36	16.52	40	27518	27150	79689680
Cutaneous sarcoidosis	27.24	16.52	9	27549	464	79716366
Mesenteric neoplasm	26.94	16.52	6	27552	66	79716764
Acute polyneuropathy	26.93	16.52	9	27549	481	79716349
Hypophysitis	26.41	16.52	17	27541	4149	79712681
Treatment failure	26.31	16.52	13	27545	170473	79546357
Vitreous floaters	26.14	16.52	21	27537	7235	79709595
Intentional overdose	26.13	16.52	3	27555	105957	79610873
Intestinal perforation	25.83	16.52	31	27527	17395	79699435
Nausea	25.53	16.52	468	27090	956728	78760102
Amylase increased	25.50	16.52	25	27533	11184	79705646
Disease progression	25.09	16.52	128	27430	184234	79532596
Gastrointestinal wall thickening	25.06	16.52	14	27544	2643	79714187
Gamma-glutamyltransferase increased	24.86	16.52	57	27501	54623	79662207
Tumour invasion	24.61	16.52	8	27550	392	79716438
Mobility decreased	24.54	16.52	6	27552	122169	79594661
Hypersensitivity	24.35	16.52	33	27525	262206	79454624
Therapy cessation	23.94	16.52	45	27513	37517	79679313
Erythema multiforme	23.90	16.52	30	27528	17621	79699209
Rhabdomyolysis	23.70	16.52	84	27474	103047	79613783
Metastatic neoplasm	23.47	16.52	17	27541	5025	79711805
Peritoneal disorder	23.36	16.52	9	27549	726	79716104
Left ventricular dysfunction	23.23	16.52	31	27527	19330	79697500
Wheezing	22.91	16.52	6	27552	116658	79600172
Chest pain	22.86	16.52	39	27519	282265	79434565
Metastases to pleura	22.76	16.52	11	27547	1543	79715287
Metastases to heart	22.71	16.52	7	27551	288	79716542
Squamous cell carcinoma of skin	22.52	16.52	26	27532	14007	79702823
Papilloedema	22.37	16.52	18	27540	6215	79710615
Pancreatitis	22.32	16.52	63	27495	68512	79648318
Autoimmune colitis	22.30	16.52	11	27547	1612	79715218
Serous retinopathy	22.14	16.52	6	27552	155	79716675
Abdominal discomfort	21.84	16.52	33	27525	250694	79466136
Cerebral haemorrhage	21.81	16.52	56	27502	57617	79659213
Ureteral disorder	21.79	16.52	8	27550	565	79716265
Rash pustular	21.68	16.52	23	27535	11288	79705542
Influenza like illness	21.53	16.52	64	27494	71643	79645187
Lymphadenopathy	21.49	16.52	53	27505	53194	79663636
General physical health deterioration	21.10	16.52	165	27393	275073	79441757
Pancreatic enzymes increased	21.01	16.52	10	27548	1355	79715475
Hypoalbuminaemia	20.95	16.52	31	27527	21266	79695564
Metastases to spleen	20.88	16.52	8	27550	636	79716194
Pain	20.88	16.52	150	27408	703652	79013178
Depression	20.41	16.52	27	27531	216763	79500067
Intentional product use issue	20.07	16.52	14	27544	152098	79564732
Macular oedema	20.06	16.52	16	27542	5458	79711372
Drug intolerance	20.03	16.52	38	27520	264081	79452749
Hepatocellular injury	19.88	16.52	48	27510	47545	79669285
Hepatotoxicity	19.56	16.52	50	27508	51302	79665528
Tumour haemorrhage	19.35	16.52	14	27544	4130	79712700
Transaminases increased	19.31	16.52	50	27508	51693	79665137
Chest discomfort	19.17	16.52	12	27546	138032	79578798
Xerosis	19.07	16.52	9	27549	1197	79715633
COVID-19	18.91	16.52	16	27542	157658	79559172
Brain neoplasm malignant	18.86	16.52	10	27548	1703	79715127
Hyperthermia	18.82	16.52	27	27531	18010	79698820
Psoriasis	18.79	16.52	4	27554	89583	79627247
Discomfort	18.75	16.52	10	27548	125607	79591223
Liver function test increased	18.67	16.52	42	27516	39731	79677099
Sarcoid-like reaction	18.59	16.52	4	27554	37	79716793
Swelling	18.42	16.52	29	27529	216682	79500148
Asthenia	17.58	16.52	261	27297	511428	79205402
Panniculitis lobular	17.56	16.52	4	27554	49	79716781
Fatigue	17.42	16.52	432	27126	929295	78787535
Small intestine carcinoma	17.21	16.52	8	27550	1028	79715802
Leukoderma	17.16	16.52	5	27553	169	79716661
Hyperkeratosis	17.03	16.52	17	27541	7773	79709057
Hepatitis	16.98	16.52	50	27508	55677	79661153
Vitiligo	16.92	16.52	10	27548	2099	79714731
Tissue infiltration	16.89	16.52	7	27551	684	79716146
Eczema	16.87	16.52	41	27517	40777	79676053
Suicide attempt	16.79	16.52	4	27554	82928	79633902
Protein S increased	16.76	16.52	3	27555	9	79716821
Infective glossitis	16.75	16.52	4	27554	61	79716769
Intentional product misuse	16.69	16.52	6	27552	95159	79621671

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EE01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Mitogen-activated protein kinase (MEK) inhibitors
FDA MoA	N0000175076	Protein Kinase Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:79091	MEK inhibitor
CHEBI has role	CHEBI:149553	anticoronaviral drug
CHEBI has role	CHEBI:176497	geroprotectors

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID
Locally advanced or metastatic anaplastic thyroid cancer (ATC) with BRAF V600E mutation	indication	255031003
Metastatic malignant melanoma	indication	443493003
Malignant Melanoma with BRAF V600E Mutation	indication	830150003
Malignant Melanoma with BRAF V600K Mutation	indication
Metastatic non-small cell lung cancer (NSCLC) with BRAF V600E mutation	indication
Unresectable or metastatic solid tumors with BRAF V600E mutation	indication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8835443	June 10, 2025	IN COMBINATION WITH DABRAFENIB FOR THE TREATMENT OF UNRESECTABLE OR METASTATIC MELANOMA.
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8835443	June 10, 2025	MEKINIST IS INDICATED, AS A SINGLE AGENT OR IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8835443	June 10, 2025	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8835443	June 10, 2025	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8835443	June 10, 2025	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8835443	June 10, 2025	TREATMENT OF UNRESECTABLE OR METASTATIC MELANOMA
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	8835443	June 10, 2025	IN COMBINATION WITH DABRAFENIB FOR THE TREATMENT OF UNRESECTABLE OR METASTATIC MELANOMA.
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	8835443	June 10, 2025	MEKINIST IS INDICATED, AS A SINGLE AGENT OR IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	8835443	June 10, 2025	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	8835443	June 10, 2025	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	8835443	June 10, 2025	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	8835443	June 10, 2025	TREATMENT OF UNRESECTABLE OR METASTATIC MELANOMA
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8835443	June 10, 2025	IN COMBINATION WITH DABRAFENIB FOR THE TREATMENT OF UNRESECTABLE OR METASTATIC MELANOMA.
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8835443	June 10, 2025	MEKINIST IS INDICATED, AS A SINGLE AGENT OR IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8835443	June 10, 2025	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8835443	June 10, 2025	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8835443	June 10, 2025	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8835443	June 10, 2025	TREATMENT OF UNRESECTABLE OR METASTATIC MELANOMA
EQ 0.05MG BASE/ML	MEKINIST	NOVARTIS	N217513	March 16, 2023	RX	SOLUTION	ORAL	8835443	June 10, 2025	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA (LGG) WITH A BRAF V600E MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8703781	Oct. 15, 2030	MEKINIST IN COMBINATION WITH DABRAFENIB FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8703781	Oct. 15, 2030	MEKINIST IS INDICATED, AS A SINGLE AGENT OR IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8703781	Oct. 15, 2030	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8703781	Oct. 15, 2030	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8703781	Oct. 15, 2030	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8952018	Oct. 15, 2030	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	8703781	Oct. 15, 2030	MEKINIST IN COMBINATION WITH DABRAFENIB FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	8703781	Oct. 15, 2030	MEKINIST IS INDICATED, AS A SINGLE AGENT OR IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	8703781	Oct. 15, 2030	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	8703781	Oct. 15, 2030	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	8703781	Oct. 15, 2030	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	8952018	Oct. 15, 2030	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8703781	Oct. 15, 2030	MEKINIST IN COMBINATION WITH DABRAFENIB FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8703781	Oct. 15, 2030	MEKINIST IS INDICATED, AS A SINGLE AGENT OR IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8703781	Oct. 15, 2030	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8703781	Oct. 15, 2030	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8703781	Oct. 15, 2030	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8952018	Oct. 15, 2030	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 0.05MG BASE/ML	MEKINIST	NOVARTIS	N217513	March 16, 2023	RX	SOLUTION	ORAL	8703781	Oct. 15, 2030	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA (LGG) WITH A BRAF V600E MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	10869869	Aug. 30, 2033	MEKINIST(R) IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	10869869	Aug. 30, 2033	MEKINIST(R) IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	10869869	Aug. 30, 2033	MEKINIST(R) IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	June 22, 2024	TRAMETINIB IN COMBINATION WITH DABRAFENIB, FOR THE TX. OF PTS WITH METASTATIC NON-SMALL CELL LUNG CANCER WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	June 22, 2024	TRAMETINIB IN COMBINATION WITH DABRAFENIB, FOR THE TX. OF PTS WITH METASTATIC NON-SMALL CELL LUNG CANCER WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	June 22, 2024	TRAMETINIB IN COMBINATION WITH DABRAFENIB, FOR THE TX. OF PTS WITH METASTATIC NON-SMALL CELL LUNG CANCER WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	Dec. 22, 2024	PEDIATRIC EXCLUSIVITY
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	Dec. 22, 2024	PEDIATRIC EXCLUSIVITY
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	Dec. 22, 2024	PEDIATRIC EXCLUSIVITY
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	April 30, 2025	TRAMETINIB IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	April 30, 2025	TRAMETINIB IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	April 30, 2025	TRAMETINIB IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	May 4, 2025	TRAMETINIB AND DABRAFENIB IN COMBINATION, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	May 4, 2025	TRAMETINIB AND DABRAFENIB IN COMBINATION, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	May 4, 2025	TRAMETINIB AND DABRAFENIB IN COMBINATION, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	June 22, 2025	TRAMETINIB IS INDICATED IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 6 YEARS OF AGE AND OLDER WITH UNRESECTABLE OR METASTATIC SOLID TUMORS WITH BRAF V600E MUTATION WHO HAVE PROGRESSED FOLLOWING PRIOR TREATMENT AND HAVE NO SATISFACTORY ALTERNATIVE TREATMENT OPTIONS
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	June 22, 2025	TRAMETINIB IS INDICATED IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 6 YEARS OF AGE AND OLDER WITH UNRESECTABLE OR METASTATIC SOLID TUMORS WITH BRAF V600E MUTATION WHO HAVE PROGRESSED FOLLOWING PRIOR TREATMENT AND HAVE NO SATISFACTORY ALTERNATIVE TREATMENT OPTIONS
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	June 22, 2025	TRAMETINIB IS INDICATED IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 6 YEARS OF AGE AND OLDER WITH UNRESECTABLE OR METASTATIC SOLID TUMORS WITH BRAF V600E MUTATION WHO HAVE PROGRESSED FOLLOWING PRIOR TREATMENT AND HAVE NO SATISFACTORY ALTERNATIVE TREATMENT OPTIONS
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	Oct. 30, 2025	PEDIATRIC EXCLUSIVITY
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	Oct. 30, 2025	PEDIATRIC EXCLUSIVITY
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	Oct. 30, 2025	PEDIATRIC EXCLUSIVITY
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	Nov. 4, 2025	PEDIATRIC EXCLUSIVITY
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	Nov. 4, 2025	PEDIATRIC EXCLUSIVITY
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	Nov. 4, 2025	PEDIATRIC EXCLUSIVITY
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	Dec. 22, 2025	PEDIATRIC EXCLUSIVITY
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	Dec. 22, 2025	PEDIATRIC EXCLUSIVITY
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	Dec. 22, 2025	PEDIATRIC EXCLUSIVITY
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	March 16, 2026	TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA WITH A BRAF V600 MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	March 16, 2026	TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA WITH A BRAF V600 MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	March 16, 2026	TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA WITH A BRAF V600 MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 0.05MG BASE/ML	MEKINIST	NOVARTIS	N217513	March 16, 2023	RX	SOLUTION	ORAL	March 16, 2026	NEW PRODUCT
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	March 16, 2030	TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA (LGG) WITH A BRAF V600E MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 1MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	DISCN	TABLET	ORAL	March 16, 2030	TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA (LGG) WITH A BRAF V600E MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 2MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	March 16, 2030	TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA (LGG) WITH A BRAF V600E MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 0.05MG BASE/ML	MEKINIST	NOVARTIS	N217513	March 16, 2023	RX	SOLUTION	ORAL	March 16, 2030	TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA (LGG) WITH A BRAF V600E MUTATION WHO REQUIRE SYSTEMIC THERAPY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Dual specificity mitogen-activated protein kinase kinase 2	Kinase	P36507	MP2K2_HUMAN	INHIBITOR	IC50	9.04	WOMBAT-PK	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 1	Kinase	Q02750	MP2K1_HUMAN	INHIBITOR	IC50	8.75	WOMBAT-PK	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		EC50	6.61	CHEMBL

External reference:

ID	Source
D10175	KEGG_DRUG
1187431-43-1	SECONDARY_CAS_RN
4032511	VANDF
CHEBI:75998	CHEBI
QOM	PDB_CHEM_ID
CHEMBL2103875	ChEMBL_ID
CHEMBL2105741	ChEMBL_ID
C560077	MESH_SUPPLEMENTAL_RECORD_UI
6495	IUPHAR_LIGAND_ID
9421	INN_ID
DB08911	DRUGBANK_ID
33E86K87QN	UNII
1425098	RXNORM
203115	MMSL
29478	MMSL
41325	MMSL
d08104	MMSL
015044	NDDF
015045	NDDF
708711009	SNOMEDCT_US
715545006	SNOMEDCT_US
734611008	SNOMEDCT_US
C2697961	UMLSCUI
11707110	PUBCHEM_CID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0666	TABLET, FILM COATED	0.50 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0666	TABLET, FILM COATED	0.50 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0666	TABLET, FILM COATED	0.50 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0666	TABLET, FILM COATED	0.50 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0668	TABLET, FILM COATED	2 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0668	TABLET, FILM COATED	2 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0668	TABLET, FILM COATED	2 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0668	TABLET, FILM COATED	2 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1105	TABLET, FILM COATED	0.50 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1105	TABLET, FILM COATED	0.50 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1105	TABLET, FILM COATED	0.50 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1105	TABLET, FILM COATED	0.50 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1112	TABLET, FILM COATED	2 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1112	TABLET, FILM COATED	2 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1112	TABLET, FILM COATED	2 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1112	TABLET, FILM COATED	2 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1161	POWDER, FOR SOLUTION	0.05 mg	ORAL	NDA	32 sections