tofacitinib Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
Janus kinase inhibitors, antineoplastics	4713	477600-75-2

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: tasocitinib xeljanz CP 690550 tofacitinib citrate tofacitinib CP-690550

Tofacitinib is a Janus kinase (JAK) inhibitor. JAKs are intracellular enzymes which transmit signals arising from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoiesis and immune cell function. Within the signaling pathway, JAKs phosphorylate and activate Signal Transducers and Activators of Transcription (STATs) which modulate intracellular activity including gene expression. Tofacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs. Molecular weight: 312.38 Formula: C16H20N6O CLOGP: 1.55 LIPINSKI: 0 HAC: 7 HDO: 1 TPSA: 88.91 ALOGS: -3.02 ROTB: 3 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	1.24 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	5.88 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.60 %	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Nov. 6, 2012	FDA	PF PRISM CV

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
Drug ineffective	10596.72	37.49	4210	19553	97414	2236908
Arthralgia	7068.66	37.49	2668	21095	51617	2282705
Condition aggravated	5224.53	37.49	1866	21897	30113	2304209
Joint swelling	4940.07	37.49	1530	22233	15289	2319033
Pain	4697.15	37.49	2073	21690	59784	2274538
Musculoskeletal stiffness	4631.76	37.49	1355	22408	10892	2323430
Rheumatoid arthritis	4171.85	37.49	1389	22374	17751	2316571
Fatigue	3456.94	37.49	1861	21902	83012	2251310
Synovitis	3354.60	37.49	773	22990	1953	2332369
Headache	3344.35	37.49	1787	21976	78392	2255930
Pain in extremity	3138.26	37.49	1403	22360	41137	2293185
Peripheral swelling	3120.85	37.49	1096	22667	16501	2317821
Therapeutic product effect incomplete	2432.90	37.49	801	22962	9730	2324592
Nasopharyngitis	2216.05	37.49	908	22855	21148	2313174
Malaise	2096.24	37.49	1164	22599	54421	2279901
Herpes zoster	1917.14	37.49	657	23106	9068	2325254
Nausea	1628.38	37.49	1294	22469	110895	2223427
Infection	1575.72	37.49	673	23090	17356	2316966
Abdominal discomfort	1543.26	37.49	657	23106	16799	2317523
Sinusitis	1534.16	37.49	644	23119	15882	2318440
Diarrhoea	1505.68	37.49	1098	22665	82466	2251856
Rash	1464.92	37.49	949	22814	58609	2275713
Swelling	1400.67	37.49	602	23161	15748	2318574
Joint range of motion decreased	1388.63	37.49	353	23410	1503	2332819
Urinary tract infection	1329.71	37.49	701	23062	29241	2305081
Musculoskeletal pain	1324.81	37.49	515	23248	10315	2324007
Cough	1310.34	37.49	718	23045	32399	2301923
Drug intolerance	1293.95	37.49	541	23222	13176	2321146
Blood cholesterol increased	1281.71	37.49	417	23346	4824	2329498
Product dose omission	1258.63	37.49	735	23028	37522	2296800
Weight increased	1244.92	37.49	610	23153	21727	2312595
Upper respiratory tract infection	1240.80	37.49	465	23298	8386	2325936
Back pain	1237.31	37.49	681	23082	30978	2303344
Contraindicated product administered	1209.37	37.49	351	23412	2670	2331652
Loss of personal independence in daily activities	1175.76	37.49	392	23371	4919	2329403
Alopecia	1116.70	37.49	564	23199	21437	2312885
Arthropathy	1115.68	37.49	409	23354	6907	2327415
Pneumonia	1106.45	37.49	743	23020	48553	2285769
Joint stiffness	1093.60	37.49	347	23416	3676	2330646
Influenza	1068.45	37.49	465	23298	12513	2321809
Tenderness	1055.64	37.49	286	23477	1632	2332690
Fall	994.79	37.49	684	23079	46415	2287907
Therapeutic product effect decreased	981.53	37.49	415	23348	10374	2323948
Treatment failure	940.62	37.49	360	23403	6879	2327443
Bronchitis	938.98	37.49	432	23331	13282	2321040
Oropharyngeal pain	935.80	37.49	409	23354	11109	2323213
Abdominal pain upper	908.02	37.49	492	23271	21608	2312714
Rhinorrhoea	843.69	37.49	336	23427	7164	2327158
Product use issue	834.93	37.49	384	23379	11785	2322537
Arthritis	812.87	37.49	355	23408	9613	2324709
Dry mouth	778.81	37.49	326	23437	7927	2326395
Drug hypersensitivity	737.33	37.49	569	23194	46074	2288248
Gait disturbance	736.29	37.49	432	23331	22113	2312209
Dry eye	734.13	37.49	256	23507	3700	2330622
Fibromyalgia	680.09	37.49	231	23532	3069	2331253
Neck pain	672.77	37.49	288	23475	7409	2326913
Hepatic enzyme increased	649.25	37.49	302	23461	9500	2324822
Myalgia	645.42	37.49	402	23361	22931	2311391
C-reactive protein abnormal	631.97	37.49	159	23604	640	2333682
Insomnia	630.57	37.49	411	23352	25376	2308946
Muscle spasms	625.49	37.49	383	23380	21183	2313139
Tuberculin test positive	625.48	37.49	149	23614	449	2333873
Dyspepsia	601.80	37.49	287	23476	9557	2324765
Osteoporosis	581.87	37.49	222	23541	4192	2330130
Blood pressure increased	576.68	37.49	334	23429	16652	2317670
Nasal congestion	573.77	37.49	250	23513	6716	2327606
Dizziness	567.02	37.49	540	23223	58125	2276197
Hypoaesthesia	513.05	37.49	330	23433	19885	2314437
Osteoarthritis	510.01	37.49	230	23533	6716	2327606
Hand deformity	509.79	37.49	143	23620	943	2333379
Abdominal pain	500.49	37.49	400	23363	33974	2300348
Grip strength decreased	499.89	37.49	140	23623	917	2333405
Dyspnoea	489.80	37.49	573	23190	78160	2256162
Contusion	486.08	37.49	271	23492	12539	2321783
Red blood cell sedimentation rate abnormal	473.46	37.49	116	23647	407	2333915
Joint effusion	465.10	37.49	138	23625	1138	2333184
Constipation	461.63	37.49	317	23446	21312	2313010
Liver function test increased	459.66	37.49	170	23593	2931	2331391
Red blood cell sedimentation rate increased	453.59	37.49	153	23610	1984	2332338
Therapeutic response unexpected	440.92	37.49	175	23588	3684	2330638
Pyrexia	436.16	37.49	450	23313	53258	2281064
Asthenia	435.88	37.49	423	23340	46503	2287819
Nodule	435.78	37.49	150	23613	2076	2332246
Hypersensitivity	429.95	37.49	314	23449	23279	2311043
Sensitivity to weather change	424.65	37.49	104	23659	364	2333958
Gastrointestinal disorder	423.30	37.49	219	23544	8698	2325624
Pre-existing condition improved	419.95	37.49	106	23657	433	2333889
Sleep disorder	414.17	37.49	195	23568	6294	2328028
Foot deformity	412.67	37.49	140	23623	1849	2332473
Paraesthesia	407.04	37.49	296	23467	21792	2312530
Depression	406.30	37.49	326	23437	27806	2306516
Gastric disorder	405.65	37.49	163	23600	3547	2330775
Therapy cessation	403.64	37.49	179	23584	5014	2329308
Hypertension	399.25	37.49	319	23444	27042	2307280
Product use in unapproved indication	395.21	37.49	226	23537	10974	2323348
Vomiting	389.14	37.49	487	23276	71115	2263207
Joint noise	385.38	37.49	102	23661	522	2333800
Feeling abnormal	385.31	37.49	294	23469	23287	2311035
Intentional product misuse	379.75	37.49	208	23555	9281	2325041
Bone erosion	366.22	37.49	96	23667	470	2333852
Acne	366.20	37.49	145	23618	3031	2331291
Cystitis	358.34	37.49	169	23594	5473	2328849
Diverticulitis	347.74	37.49	151	23612	4014	2330308
Mobility decreased	338.44	37.49	188	23575	8622	2325700
C-reactive protein increased	332.86	37.49	166	23597	6089	2328233
Stress	325.19	37.49	169	23594	6769	2327553
Pruritus	322.67	37.49	347	23416	42993	2291329
Inflammation	310.41	37.49	158	23605	6055	2328267
Crepitations	300.29	37.49	85	23678	581	2333741
Anxiety	297.49	37.49	278	23485	29081	2305241
Femur fracture	292.65	37.49	156	23607	6583	2327739
Immune system disorder	286.49	37.49	98	23665	1328	2332994
Localised infection	285.74	37.49	118	23645	2758	2331564
Abdominal distension	281.30	37.49	177	23586	10234	2324088
Viral infection	278.39	37.49	134	23629	4542	2329780
Bursitis	276.82	37.49	103	23660	1805	2332517
Off label use	273.48	37.49	417	23346	73181	2261141
Memory impairment	272.09	37.49	188	23575	12735	2321587
Drug effective for unapproved indication	270.53	37.49	64	23699	185	2334137
Cataract	265.67	37.49	140	23623	5768	2328554
Mycobacterium tuberculosis complex test positive	265.12	37.49	70	23693	354	2333968
Fungal infection	263.79	37.49	131	23632	4758	2329564
Sinus disorder	263.09	37.49	109	23654	2569	2331753
Lower respiratory tract infection	259.54	37.49	134	23629	5290	2329032
Nail disorder	255.55	37.49	85	23678	1051	2333271
Gastrooesophageal reflux disease	254.18	37.49	158	23605	8937	2325385
Mouth ulceration	253.96	37.49	119	23644	3793	2330529
Ear infection	252.59	37.49	114	23649	3327	2330995
Rheumatoid nodule	247.85	37.49	72	23691	546	2333776
Joint injury	246.05	37.49	101	23662	2323	2331999
Weight decreased	242.92	37.49	245	23518	28126	2306196
Carpal tunnel syndrome	242.33	37.49	95	23668	1930	2332392
Onychomycosis	240.49	37.49	69	23694	498	2333824
Interstitial lung disease	236.92	37.49	143	23620	7669	2326653
Joint laxity	230.51	37.49	44	23719	18	2334304
Erythema	229.66	37.49	225	23538	24934	2309388
Muscular weakness	228.39	37.49	179	23584	14718	2319604
Disease recurrence	224.08	37.49	105	23658	3346	2330976
Lung disorder	223.40	37.49	127	23636	6085	2328237
Oral herpes	220.95	37.49	91	23672	2111	2332211
Soft tissue disorder	219.13	37.49	54	23709	195	2334127
Adverse drug reaction	216.66	37.49	138	23625	8145	2326177
Rheumatoid factor positive	215.78	37.49	62	23701	450	2333872
Pollakiuria	215.61	37.49	105	23658	3651	2330671
Stomatitis	215.57	37.49	146	23617	9564	2324758
Migraine	214.89	37.49	151	23612	10502	2323820
Anti-cyclic citrullinated peptide antibody positive	214.41	37.49	51	23712	152	2334170
Kidney infection	213.93	37.49	93	23670	2476	2331846
Chest pain	213.89	37.49	228	23535	27909	2306413
Chills	213.15	37.49	175	23588	15377	2318945
Limb discomfort	210.75	37.49	100	23663	3279	2331043
Intentional product use issue	210.69	37.49	102	23661	3500	2330822
Musculoskeletal discomfort	209.93	37.49	87	23676	2051	2332271
Liver function test abnormal	208.97	37.49	130	23633	7360	2326962
Influenza like illness	208.59	37.49	156	23607	11958	2322364
Synovial cyst	207.33	37.49	68	23695	802	2333520
Impaired healing	200.99	37.49	113	23650	5298	2329024
Non-Hodgkin's lymphoma	199.99	37.49	67	23696	848	2333474
Cellulitis	198.67	37.49	136	23627	9065	2325257
Anaemia	198.53	37.49	243	23520	34549	2299773
Bone disorder	197.93	37.49	95	23668	3197	2331125
Coeliac disease	194.13	37.49	64	23699	768	2333554
Impaired work ability	189.09	37.49	77	23686	1733	2332589
Night sweats	186.46	37.49	93	23670	3407	2330915
Tooth infection	186.21	37.49	78	23685	1890	2332432
Hot flush	183.45	37.49	118	23645	7081	2327241
Sjogren's syndrome	181.29	37.49	64	23699	957	2333365
Productive cough	181.20	37.49	105	23658	5216	2329106
Tuberculosis	180.77	37.49	76	23687	1859	2332463
Joint dislocation	180.19	37.49	70	23693	1386	2332936
Respiratory tract infection	179.75	37.49	95	23668	3934	2330388
Drug ineffective for unapproved indication	179.55	37.49	86	23677	2880	2331442
Nephrolithiasis	177.25	37.49	98	23665	4445	2329877
Wound	177.09	37.49	83	23680	2645	2331677
Flatulence	174.87	37.49	97	23666	4428	2329894
Synovial fluid analysis	173.01	37.49	31	23732	0	2334322
Ulcer	169.50	37.49	72	23691	1808	2332514
Synovial disorder	167.65	37.49	37	23726	69	2334253
Limb injury	164.89	37.49	77	23686	2433	2331889
Visual impairment	164.65	37.49	134	23629	11621	2322701
Neoplasm malignant	164.19	37.49	97	23666	4996	2329326
Finger deformity	158.00	37.49	55	23708	787	2333535
Eye infection	151.88	37.49	60	23703	1244	2333078
Hyperhidrosis	150.17	37.49	143	23620	15279	2319043
Poor quality sleep	150.17	37.49	67	23696	1900	2332422
Rheumatic fever	149.36	37.49	33	23730	62	2334260
Gastroenteritis viral	148.91	37.49	72	23691	2462	2331860
Tenosynovitis stenosans	148.23	37.49	35	23728	100	2334222
Skin lesion	146.60	37.49	83	23680	3942	2330380
Scleritis	146.52	37.49	41	23722	267	2334055
Therapeutic product effect variable	146.50	37.49	36	23727	128	2334194
Pelvic fracture	145.36	37.49	59	23704	1316	2333006
Gait inability	145.30	37.49	95	23668	5860	2328462
Skin disorder	143.49	37.49	79	23684	3552	2330770
Swelling face	143.11	37.49	113	23650	9380	2324942
Increased tendency to bruise	142.67	37.49	61	23702	1557	2332765
Therapeutic product effect delayed	142.64	37.49	45	23718	464	2333858
Glossodynia	141.32	37.49	64	23699	1881	2332441
Foot fracture	141.18	37.49	72	23691	2766	2331556
Pulmonary fibrosis	140.18	37.49	70	23693	2570	2331752
Surgery	139.22	37.49	90	23673	5445	2328877
Oedema peripheral	135.47	37.49	166	23597	23597	2310725
Discomfort	134.98	37.49	86	23677	5073	2329249
Oral pain	134.49	37.49	74	23689	3323	2330999
Onychomadesis	130.85	37.49	42	23721	460	2333862
Cushingoid	130.67	37.49	44	23719	566	2333756
Haematochezia	128.03	37.49	84	23679	5211	2329111
Blister	127.33	37.49	92	23671	6679	2327643
Systemic lupus erythematosus	127.23	37.49	77	23686	4144	2330178
Decreased appetite	126.15	37.49	177	23586	28714	2305608
Flank pain	125.59	37.49	55	23708	1490	2332832
Tooth abscess	124.97	37.49	60	23703	2019	2332303
Exostosis	124.97	37.49	53	23710	1325	2332997
Dry skin	124.22	37.49	90	23673	6562	2327760
Wheezing	122.93	37.49	88	23675	6296	2328026
Groin pain	122.68	37.49	52	23711	1298	2333024
Back disorder	119.84	37.49	54	23709	1568	2332754
Asthma	117.97	37.49	109	23654	11205	2323117
Leukopenia	117.66	37.49	104	23659	10092	2324230
Palpitations	117.30	37.49	129	23634	16327	2317995
Pneumonia viral	116.79	37.49	38	23725	436	2333886
Dysphonia	114.07	37.49	84	23679	6280	2328042
Burning sensation	113.32	37.49	91	23672	7737	2326585
Conjunctivitis	111.21	37.49	58	23705	2335	2331987
Tinnitus	111.03	37.49	76	23687	5059	2329263
Wrist deformity	109.92	37.49	26	23737	75	2334247
Hair growth abnormal	108.50	37.49	38	23725	554	2333768
Pemphigus	107.29	37.49	39	23724	637	2333685
Ocular hyperaemia	107.06	37.49	68	23695	3988	2330334
Upper limb fracture	106.91	37.49	59	23704	2664	2331658
Intentional dose omission	105.41	37.49	33	23730	331	2333991
Pain in jaw	105.06	37.49	80	23683	6292	2328030
Pulmonary mass	105.01	37.49	52	23711	1874	2332448
Pleuritic pain	104.97	37.49	38	23725	613	2333709
Thrombosis	104.97	37.49	93	23670	9051	2325271
Sepsis	103.48	37.49	128	23635	18360	2315962
Laryngitis	103.31	37.49	47	23716	1396	2332926
Eye disorder	102.93	37.49	61	23702	3158	2331164
Movement disorder	102.12	37.49	58	23705	2770	2331552
Feeling jittery	101.90	37.49	51	23712	1881	2332441
Extremity contracture	100.85	37.49	25	23738	93	2334229
Body height decreased	100.29	37.49	44	23719	1197	2333125
Spinal pain	100.07	37.49	45	23718	1300	2333022
Musculoskeletal disorder	99.87	37.49	55	23708	2473	2331849
Ankle fracture	99.86	37.49	53	23710	2212	2332110
Diabetes mellitus	99.81	37.49	83	23680	7412	2326910
Skin ulcer	99.61	37.49	65	23698	3994	2330328
Nodal osteoarthritis	99.55	37.49	24	23739	77	2334245
Low density lipoprotein increased	99.45	37.49	44	23719	1222	2333100
Antinuclear antibody positive	99.40	37.49	42	23721	1040	2333282
Scar	99.33	37.49	50	23713	1867	2332455
Liver disorder	98.05	37.49	77	23686	6337	2327985
Spinal stenosis	97.79	37.49	45	23718	1373	2332949
Trigger finger	96.11	37.49	33	23730	452	2333870
Knee arthroplasty	94.84	37.49	56	23707	2879	2331443
Staphylococcal infection	94.77	37.49	70	23693	5256	2329066
Renal disorder	93.67	37.49	65	23698	4423	2329899
Urticaria	93.29	37.49	140	23623	24121	2310201
Intervertebral disc degeneration	92.37	37.49	45	23718	1564	2332758
Tendonitis	92.26	37.49	50	23713	2177	2332145
Respiratory tract congestion	92.00	37.49	51	23712	2323	2331999
Epistaxis	91.98	37.49	89	23674	9690	2324632
Depressed mood	91.78	37.49	68	23695	5130	2329192
Therapeutic response decreased	90.29	37.49	77	23686	7118	2327204
Soft tissue swelling	89.99	37.49	21	23742	56	2334266
Sinus congestion	88.59	37.49	47	23716	1960	2332362
Dysstasia	86.99	37.49	53	23710	2886	2331436
Pharyngitis	86.57	37.49	48	23715	2187	2332135
Eye irritation	85.59	37.49	56	23707	3456	2330866
Fungal skin infection	85.47	37.49	31	23732	503	2333819
Dysuria	84.42	37.49	58	23705	3883	2330439
Pustular psoriasis	83.49	37.49	35	23728	849	2333473
Muscle fatigue	83.44	37.49	28	23735	356	2333966
Sciatica	83.31	37.49	46	23717	2079	2332243
Skin discolouration	82.70	37.49	65	23698	5355	2328967
Feeling hot	82.59	37.49	72	23691	6856	2327466
Throat irritation	82.58	37.49	63	23700	4967	2329355
Psoriasis	81.42	37.49	109	23654	16899	2317423
Intervertebral disc protrusion	80.30	37.49	51	23712	2990	2331332
Blood glucose increased	80.13	37.49	92	23671	12198	2322124
Hip arthroplasty	79.79	37.49	43	23720	1851	2332471
Wound infection	79.79	37.49	38	23725	1255	2333067
Road traffic accident	79.76	37.49	58	23705	4250	2330072
Viral upper respiratory tract infection	79.76	37.49	36	23727	1049	2333273
Eye pain	79.73	37.49	61	23702	4830	2329492
Arthritis bacterial	79.32	37.49	33	23730	785	2333537
Multiple fractures	79.30	37.49	31	23732	624	2333698
Neuralgia	78.71	37.49	49	23714	2773	2331549
White blood cell count decreased	78.60	37.49	111	23652	18097	2316225
Prescribed overdose	78.49	37.49	42	23721	1782	2332540
Iron deficiency anaemia	78.36	37.49	44	23719	2055	2332267
Vision blurred	77.98	37.49	99	23664	14569	2319753
Ill-defined disorder	77.80	37.49	52	23711	3326	2330996
Rib fracture	77.49	37.49	47	23716	2538	2331784
Skin cancer	77.27	37.49	41	23722	1710	2332612
Lipids increased	76.54	37.49	24	23739	242	2334080
Toothache	76.51	37.49	47	23716	2597	2331725
Amnesia	75.82	37.49	70	23693	7183	2327139
Rotator cuff syndrome	75.67	37.49	41	23722	1784	2332538
Hepatitis B virus test positive	75.33	37.49	18	23745	55	2334267
Renal impairment	75.17	37.49	81	23682	10011	2324311
Photophobia	74.81	37.49	44	23719	2245	2332077
Injection site reaction	74.40	37.49	98	23665	14954	2319368
Blood creatinine increased	74.04	37.49	82	23681	10451	2323871
Lymphadenopathy	73.58	37.49	62	23701	5636	2328686
Red blood cell count decreased	73.50	37.49	55	23708	4211	2330111
Pericarditis	73.49	37.49	38	23725	1502	2332820
Temperature intolerance	73.04	37.49	33	23730	964	2333358
Blood triglycerides increased	73.00	37.49	43	23720	2200	2332122
Inflammatory marker increased	72.45	37.49	28	23735	546	2333776
Ear pain	72.33	37.49	46	23717	2703	2331619
Seasonal allergy	71.46	37.49	38	23725	1592	2332730
Deafness	70.57	37.49	45	23718	2656	2331666
Hepatic steatosis	70.51	37.49	48	23715	3165	2331157
Heart rate increased	70.50	37.49	82	23681	11023	2323299
Lung neoplasm malignant	70.47	37.49	47	23716	2995	2331327
Hypoacusis	70.06	37.49	49	23714	3376	2330946
Skin infection	69.83	37.49	36	23727	1414	2332908
Middle insomnia	69.20	37.49	36	23727	1441	2332881
Post procedural infection	69.20	37.49	33	23730	1093	2333229
Arthritis infective	69.11	37.49	28	23735	621	2333701
Deformity	69.04	37.49	26	23737	471	2333851
Dysphagia	68.98	37.49	87	23676	12718	2321604
Skin papilloma	68.59	37.49	27	23736	554	2333768
Immunosuppression	67.75	37.49	32	23731	1037	2333285
Balance disorder	66.99	37.49	75	23688	9672	2324650
Hip fracture	66.53	37.49	54	23709	4658	2329664
Lower limb fracture	65.39	37.49	39	23724	2042	2332280
Meniscus injury	63.90	37.49	31	23732	1067	2333255
Tendon rupture	62.65	37.49	34	23729	1484	2332838
Walking aid user	62.21	37.49	27	23736	715	2333607
Atelectasis	62.20	37.49	37	23726	1928	2332394
Colon cancer	61.20	37.49	36	23727	1837	2332485
Herpes virus infection	61.03	37.49	28	23735	848	2333474
Pulmonary embolism	60.62	37.49	98	23665	17985	2316337
Haemoglobin decreased	60.35	37.49	98	23665	18053	2316269
Upper-airway cough syndrome	60.30	37.49	29	23734	979	2333343
Furuncle	60.13	37.49	29	23734	985	2333337
Incorrect dosage administered	60.09	37.49	22	23741	367	2333955
Concussion	59.81	37.49	28	23735	889	2333433
Bone pain	59.74	37.49	68	23695	8928	2325394
Adverse event	59.73	37.49	63	23700	7596	2326726
Spinal fracture	59.23	37.49	41	23722	2778	2331544
Laboratory test abnormal	59.10	37.49	53	23710	5237	2329085
Aphonia	58.97	37.49	31	23732	1268	2333054
Vitamin D decreased	58.89	37.49	29	23734	1032	2333290
Osteomyelitis	58.53	37.49	45	23718	3588	2330734
Death	58.52	37.49	246	23517	81222	2253100
Type 2 diabetes mellitus	58.43	37.49	37	23726	2157	2332165
Chronic obstructive pulmonary disease	58.40	37.49	60	23703	7017	2327305
Cyst	58.40	37.49	33	23730	1560	2332762
Oedema	57.63	37.49	71	23692	10132	2324190
Colitis ulcerative	57.11	37.49	40	23723	2762	2331560
Pharyngitis streptococcal	56.51	37.49	32	23731	1519	2332803
Gastroenteritis	56.20	37.49	41	23722	3019	2331303
Thyroid disorder	56.09	37.49	32	23731	1541	2332781
Energy increased	56.09	37.49	22	23741	447	2333875
Wrist fracture	55.99	37.49	33	23730	1690	2332632
Epicondylitis	55.75	37.49	19	23744	254	2334068
Tooth disorder	55.59	37.49	46	23717	4077	2330245
Ligament sprain	55.51	37.49	31	23732	1432	2332890
Nerve compression	55.19	37.49	27	23736	947	2333375
Photosensitivity reaction	55.02	37.49	37	23726	2390	2331932
Osteopenia	54.98	37.49	34	23729	1901	2332421
Joint warmth	54.82	37.49	19	23744	268	2334054
Respiratory disorder	54.67	37.49	45	23718	3959	2330363
Rosacea	53.64	37.49	22	23741	504	2333818
Breast cancer	53.51	37.49	66	23697	9429	2324893
Menopausal symptoms	53.38	37.49	20	23743	357	2333965
Increased appetite	53.25	37.49	30	23733	1410	2332912
Blood test abnormal	52.95	37.49	29	23734	1289	2333033
Spinal disorder	52.45	37.49	28	23735	1182	2333140
Rheumatoid factor negative	52.37	37.49	11	23752	14	2334308
Gallbladder disorder	52.11	37.49	38	23725	2796	2331526
Limb deformity	52.06	37.49	18	23745	252	2334070
Somnolence	51.63	37.49	106	23657	23379	2310943
Irritable bowel syndrome	51.42	37.49	32	23731	1809	2332513
Paranasal sinus discomfort	51.42	37.49	20	23743	397	2333925
White blood cell count increased	51.29	37.49	56	23707	7022	2327300
Tremor	51.13	37.49	98	23665	20563	2313759
Blood pressure abnormal	51.10	37.49	31	23732	1674	2332648
Bacterial infection	50.69	37.49	34	23729	2187	2332135
Sputum discoloured	50.59	37.49	27	23736	1139	2333183
Immobile	50.53	37.49	22	23741	587	2333735
Cerebrovascular accident	50.27	37.49	96	23667	20090	2314232
Decreased immune responsiveness	50.24	37.49	23	23740	693	2333629
Haemorrhage	50.16	37.49	69	23694	10970	2323352
Rash papular	49.86	37.49	36	23727	2608	2331714
Fluid retention	49.76	37.49	55	23708	6991	2327331
Onychoclasis	49.63	37.49	24	23739	820	2333502
Intervertebral disc disorder	49.45	37.49	22	23741	619	2333703
Joint lock	49.09	37.49	19	23744	372	2333950
Nervousness	48.35	37.49	47	23716	5142	2329180
Cardiac disorder	48.31	37.49	57	23706	7776	2326546
Myocardial infarction	48.06	37.49	91	23672	18922	2315400
Adverse reaction	47.99	37.49	29	23734	1555	2332767
Oral discomfort	47.78	37.49	27	23736	1276	2333046
Bone swelling	47.78	37.49	16	23747	202	2334120
Sleep apnoea syndrome	47.21	37.49	32	23731	2094	2332228
Sinusitis bacterial	47.08	37.49	13	23750	80	2334242
Clostridium difficile infection	47.00	37.49	36	23727	2854	2331468
Therapy non-responder	46.75	37.49	57	23706	8047	2326275
Atrial fibrillation	46.66	37.49	75	23688	13693	2320629
Raynaud's phenomenon	46.52	37.49	24	23739	944	2333378
Rheumatoid factor increased	46.40	37.49	16	23747	222	2334100
Nerve injury	46.24	37.49	25	23738	1083	2333239
Alanine aminotransferase increased	45.60	37.49	75	23688	13957	2320365
Dry throat	45.60	37.49	24	23739	984	2333338
Food poisoning	44.82	37.49	19	23744	474	2333848
Lymphoma	44.80	37.49	30	23733	1924	2332398
Tendon disorder	44.38	37.49	22	23741	794	2333528
Hunger	44.19	37.49	21	23742	690	2333632
Upper respiratory tract congestion	44.11	37.49	18	23745	407	2333915
Sneezing	43.64	37.49	32	23731	2374	2331948
Gingival bleeding	43.43	37.49	30	23733	2025	2332297
Skin atrophy	43.01	37.49	20	23743	625	2333697
Oral mucosal blistering	42.88	37.49	22	23741	855	2333467
Candida infection	42.84	37.49	34	23729	2839	2331483
Bone cyst	42.76	37.49	14	23749	164	2334158
Chondropathy	42.64	37.49	17	23746	361	2333961
Sinus pain	42.60	37.49	14	23749	166	2334156
General physical health deterioration	42.53	37.49	73	23690	14066	2320256
Rotator cuff repair	42.25	37.49	15	23748	228	2334094
Chest discomfort	42.13	37.49	74	23689	14521	2319801
Ear discomfort	42.06	37.49	24	23739	1156	2333166
Injection site hypersensitivity	41.43	37.49	17	23746	390	2333932
Crying	41.30	37.49	40	23723	4356	2329966
Hepatotoxicity	41.12	37.49	36	23727	3445	2330877
Helicobacter infection	41.00	37.49	19	23744	589	2333733
Ophthalmic herpes zoster	40.88	37.49	16	23747	323	2333999
Tenosynovitis	40.74	37.49	18	23745	498	2333824
Muscle strain	40.72	37.49	23	23740	1086	2333236
Glaucoma	40.59	37.49	29	23734	2066	2332256
Enteritis infectious	40.23	37.49	15	23748	264	2334058
Butterfly rash	40.10	37.49	14	23749	202	2334120
Fracture	40.04	37.49	32	23731	2699	2331623
Joint contracture	39.85	37.49	14	23749	206	2334116
Swollen joint count increased	39.62	37.49	8	23755	7	2334315
Skin mass	39.26	37.49	22	23741	1023	2333299
Granulomatous rosacea	39.06	37.49	7	23756	0	2334322
Nail growth abnormal	38.72	37.49	12	23751	116	2334206
High density lipoprotein increased	38.61	37.49	13	23750	167	2334155
Muscle tightness	38.37	37.49	27	23736	1878	2332444
Spinal operation	38.31	37.49	20	23743	806	2333516
Blood urine present	38.28	37.49	27	23736	1885	2332437
Fine motor skill dysfunction	38.23	37.49	15	23748	305	2334017
Red cell distribution width increased	38.06	37.49	18	23745	585	2333737
Breast mass	37.55	37.49	22	23741	1114	2333208
Pain of skin	37.52	37.49	24	23739	1424	2332898

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
Drug ineffective	2238.50	45.82	924	4585	62877	1678395
Arthralgia	1429.13	45.82	513	4996	22931	1718341
Joint swelling	1292.88	45.82	351	5158	6002	1735270
Musculoskeletal stiffness	1034.14	45.82	290	5219	5586	1735686
Pain	943.01	45.82	394	5115	26263	1715009
Condition aggravated	931.00	45.82	366	5143	20784	1720488
Rheumatoid arthritis	804.31	45.82	226	5283	4359	1736913
Peripheral swelling	685.08	45.82	227	5282	7744	1733528
Therapeutic product effect incomplete	593.83	45.82	186	5323	5262	1736010
Pain in extremity	560.87	45.82	246	5263	18226	1723046
Synovitis	532.88	45.82	114	5395	631	1740641
Fatigue	510.73	45.82	322	5187	50459	1690813
Joint range of motion decreased	413.79	45.82	94	5415	712	1740560
Herpes zoster	411.08	45.82	135	5374	4438	1736834
Headache	364.26	45.82	226	5283	34150	1707122
Loss of personal independence in daily activities	294.92	45.82	90	5419	2309	1738963
Musculoskeletal pain	294.02	45.82	108	5401	4966	1736306
Malaise	247.59	45.82	168	5341	29397	1711875
Pneumonia	242.33	45.82	198	5311	45984	1695288
Back pain	240.45	45.82	134	5375	16479	1724793
Nasopharyngitis	238.47	45.82	113	5396	9897	1731375
Contraindicated product administered	233.48	45.82	67	5442	1377	1739895
Infection	227.39	45.82	117	5392	12243	1729029
Swelling	226.96	45.82	98	5411	6898	1734374
Product use issue	220.30	45.82	102	5407	8469	1732803
Diarrhoea	211.95	45.82	196	5313	53656	1687616
Product dose omission	200.76	45.82	133	5376	22307	1718965
Drug effective for unapproved indication	198.24	45.82	39	5470	129	1741143
Mobility decreased	197.92	45.82	76	5433	3944	1737328
Sinusitis	195.42	45.82	81	5428	5142	1736130
Mass	189.31	45.82	54	5455	1084	1740188
Joint stiffness	186.93	45.82	59	5450	1692	1739580
Cough	184.38	45.82	119	5390	19078	1722194
Dyspnoea	182.78	45.82	178	5331	51881	1689391
Arthropathy	180.72	45.82	65	5444	2802	1738470
Product use in unapproved indication	178.39	45.82	91	5418	9331	1731941
Abdominal discomfort	172.77	45.82	88	5421	8993	1732279
Treatment failure	170.53	45.82	70	5439	4331	1736941
Rash	167.88	45.82	149	5360	38544	1702728
Arthritis	166.96	45.82	67	5442	3908	1737364
Limb discomfort	164.33	45.82	51	5458	1381	1739891
Influenza	159.78	45.82	76	5433	6691	1734581
Osteoarthritis	159.65	45.82	56	5453	2240	1739032
Diverticulitis	155.15	45.82	55	5454	2270	1739002
Tenderness	154.26	45.82	45	5464	980	1740292
Therapeutic product effect decreased	152.58	45.82	72	5437	6225	1735047
Red blood cell sedimentation rate increased	151.41	45.82	45	5464	1048	1740224
Rhinorrhoea	143.93	45.82	60	5449	3857	1737415
Upper respiratory tract infection	141.39	45.82	60	5449	4033	1737239
Joint lock	136.97	45.82	30	5479	187	1741085
Nausea	134.39	45.82	150	5359	51046	1690226
Sensitivity to weather change	134.06	45.82	28	5481	134	1741138
Disability	132.56	45.82	35	5474	519	1740753
Abdominal pain upper	127.66	45.82	77	5432	10924	1730348
Therapeutic response unexpected	127.05	45.82	48	5461	2376	1738896
Drug hypersensitivity	126.21	45.82	86	5423	15049	1726223
Liver function test increased	120.38	45.82	41	5468	1498	1739774
Blood cholesterol increased	120.13	45.82	49	5460	2977	1738295
Drug ineffective for unapproved indication	117.21	45.82	42	5467	1787	1739485
Tuberculin test positive	114.88	45.82	29	5480	356	1740916
C-reactive protein abnormal	114.86	45.82	27	5482	240	1741032
Mycobacterium tuberculosis complex test positive	114.23	45.82	28	5481	302	1740970
Hypoaesthesia	111.92	45.82	68	5441	9767	1731505
Hypertension	111.19	45.82	88	5421	19360	1721912
Weight increased	107.83	45.82	70	5439	11287	1729985
Interstitial lung disease	107.66	45.82	66	5443	9630	1731642
Physical disability	107.06	45.82	23	5486	129	1741143
C-reactive protein increased	105.95	45.82	55	5454	5830	1735442
Nasal congestion	105.40	45.82	45	5464	3066	1738206
Depression	105.22	45.82	80	5429	16589	1724683
Pre-existing condition improved	103.34	45.82	25	5484	254	1741018
Neck pain	98.77	45.82	44	5465	3322	1737950
Skin mass	97.77	45.82	28	5481	569	1740703
Blood pressure increased	96.51	45.82	64	5445	10689	1730583
Drug intolerance	95.96	45.82	52	5457	6010	1735262
Joint noise	95.42	45.82	22	5487	178	1741094
Oropharyngeal pain	95.34	45.82	48	5461	4770	1736502
Joint effusion	93.49	45.82	27	5482	566	1740706
Hepatic enzyme increased	91.67	45.82	52	5457	6569	1734703
Myalgia	89.76	45.82	71	5438	15587	1725685
Gait disturbance	87.02	45.82	64	5445	12606	1728666
Rheumatoid factor positive	86.67	45.82	17	5492	55	1741217
Pulmonary embolism	85.29	45.82	64	5445	12995	1728277
Bronchitis	84.31	45.82	46	5463	5386	1735886
Off label use	84.22	45.82	103	5406	38468	1702804
Gastric disorder	83.47	45.82	33	5476	1845	1739427
Acne	81.16	45.82	32	5477	1776	1739496
Dry mouth	80.40	45.82	40	5469	3873	1737399
Ill-defined disorder	79.93	45.82	32	5477	1849	1739423
Therapy cessation	79.37	45.82	37	5472	3102	1738170
Insomnia	76.94	45.82	66	5443	16210	1725062
Hair growth abnormal	76.75	45.82	19	5490	214	1741058
Muscle spasms	75.98	45.82	57	5452	11564	1729708
Dry eye	74.51	45.82	27	5482	1185	1740087
Abdominal pain	74.05	45.82	73	5436	21417	1719855
Feeling abnormal	73.51	45.82	55	5454	11111	1730161
Chest pain	71.13	45.82	69	5440	19845	1721427
Gastrointestinal disorder	70.35	45.82	39	5470	4709	1736563
Hernia	69.97	45.82	26	5483	1226	1740046
Hip arthroplasty	69.90	45.82	23	5486	753	1740519
Haematochezia	68.96	45.82	39	5470	4893	1736379
Rheumatoid factor increased	67.08	45.82	15	5494	104	1741168
Fall	66.45	45.82	77	5432	27137	1714135
Contusion	66.29	45.82	39	5470	5270	1736002
Knee arthroplasty	65.86	45.82	23	5486	905	1740367
Pyrexia	63.61	45.82	99	5410	46301	1694971
Hand deformity	61.03	45.82	16	5493	230	1741042
Pulmonary thrombosis	60.71	45.82	21	5488	803	1740469
Sleep disorder	59.16	45.82	33	5476	4030	1737242
Grip strength decreased	58.16	45.82	17	5492	372	1740900
Therapy non-responder	55.45	45.82	37	5472	6229	1735043
Dyspepsia	55.44	45.82	34	5475	4951	1736321
Oral herpes	54.94	45.82	19	5490	726	1740546
Impaired work ability	54.55	45.82	21	5488	1092	1740180
Nephrolithiasis	54.27	45.82	31	5478	3961	1737311
Alopecia	53.33	45.82	30	5479	3723	1737549
Paraesthesia	52.67	45.82	44	5465	10407	1730865
Constipation	51.70	45.82	51	5458	14949	1726323
Nodal osteoarthritis	51.67	45.82	9	5500	11	1741261
Nodule	51.59	45.82	19	5490	873	1740399
Intentional product misuse	50.09	45.82	37	5472	7321	1733951
Lung neoplasm malignant	49.52	45.82	27	5482	3152	1738120
Productive cough	49.12	45.82	28	5481	3563	1737709
Gilbert's syndrome	48.49	45.82	11	5498	82	1741190
Prescribed overdose	48.28	45.82	22	5487	1748	1739524
Osteoporosis	47.76	45.82	21	5488	1534	1739738
Night sweats	45.95	45.82	23	5486	2253	1739019

Pharmacologic Action:

Source	Code	Description
ATC	L04AA29	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSUPPRESSANTS IMMUNOSUPPRESSANTS Selective immunosuppressants
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors
CHEBI has role	CHEBI:35842	antirheumatic drug
FDA EPC	N0000190858	Janus Kinase Inhibitor
FDA MoA	N0000190857	Janus Kinase Inhibitors

Drug Use (View source of the data)

Disease	Relation	SNOMED_ID	DOID
Rheumatoid arthritis	indication	69896004	DOID:7148

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.27	acidic
pKa2	6.48	Basic
pKa3	0.91	Basic

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 10MG BASE	XELJANZ	PF PRISM CV	N203214	May 30, 2018	RX	TABLET	ORAL	7842699	Dec. 8, 2020	TREATMENT OF ADULT PATIENTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS (UC)
EQ 5MG BASE	XELJANZ	PF PRISM CV	N203214	Nov. 6, 2012	RX	TABLET	ORAL	7091208	Dec. 8, 2020	TREATMENT OF RHEUMATOID ARTHRITIS
EQ 5MG BASE	XELJANZ	PF PRISM CV	N203214	Nov. 6, 2012	RX	TABLET	ORAL	7842699	Dec. 8, 2020	TREATMENT OF ADULT PATIENTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS (UC)
EQ 11MG BASE	XELJANZ XR	PFIZER INC	N208246	Feb. 23, 2016	RX	TABLET, EXTENDED RELEASE	ORAL	7091208	Dec. 8, 2020	TREATMENT OF RHEUMATOID ARTHRITIS
EQ 11MG BASE	XELJANZ XR	PFIZER INC	N208246	Feb. 23, 2016	RX	TABLET, EXTENDED RELEASE	ORAL	7842699	Dec. 8, 2020	TREATMENT OF ADULT PATIENTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS (UC)
EQ 22MG BASE	XELJANZ XR	PFIZER INC	N208246	Dec. 12, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	7842699	Dec. 8, 2020	TREATMENT OF ADULT PATIENTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS (UC)

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 5MG BASE	XELJANZ	PF PRISM CV	N203214	Nov. 6, 2012	RX	TABLET	ORAL	Dec. 14, 2020	TREATMENT OF ADULT PATIENTS WITH ACTIVE PSORIATIC ARTHRITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO METHOTREXATE OR OTHER NON-BIOLOGIC DISEASE-MODIFYING ANTIRHEUMATIC DRUGS
EQ 11MG BASE	XELJANZ XR	PFIZER INC	N208246	Feb. 23, 2016	RX	TABLET, EXTENDED RELEASE	ORAL	Dec. 14, 2020	TREATMENT OF ADULT PATIENTS WITH ACTIVE PSORIATIC ARTHRITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO METHOTREXATE OR OTHER NON-BIOLOGIC DISEASE-MODIFYING ANTIRHEUMATIC DRUGS
EQ 10MG BASE	XELJANZ	PF PRISM CV	N203214	May 30, 2018	RX	TABLET	ORAL	May 30, 2021	TREATMENT OF ADULT PATIENTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS (UC)
EQ 5MG BASE	XELJANZ	PF PRISM CV	N203214	Nov. 6, 2012	RX	TABLET	ORAL	May 30, 2021	TREATMENT OF ADULT PATIENTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS (UC)

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
JAK1/TYK2	Kinase	P23458 P29597	JAK1_HUMAN TYK2_HUMAN	INHIBITOR	IC50	7.46		CHEMBL	CHEMBL
JAK2/TYK2	Kinase	O60674 P29597	JAK2_HUMAN TYK2_HUMAN	INHIBITOR	IC50	6.64		CHEMBL	CHEMBL
JAK2/JAK1	Kinase	O60674 P23458	JAK1_HUMAN JAK2_HUMAN	INHIBITOR	IC50	6.39		DRUG LABEL	DRUG LABEL
JAK3/JAK1	Kinase	P23458 P52333	JAK1_HUMAN JAK3_HUMAN	INHIBITOR	IC50	7.25		DRUG LABEL	DRUG LABEL
Calcium/calmodulin-dependent protein kinase type 1	Kinase	Q14012	KCC1A_HUMAN		Kd	5.92		CHEMBL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN	INHIBITOR	Kd	9.24		CHEMBL
Ribosomal protein S6 kinase alpha-6	Kinase	Q9UK32	KS6A6_HUMAN		Kd	6.27		CHEMBL
Ribosomal protein S6 kinase alpha-1	Kinase	Q15418	KS6A1_HUMAN		Kd	5.85		CHEMBL
JAK1/JAK2/TYK2	Kinase	O60674 P23458 P29597	JAK1_HUMAN JAK2_HUMAN TYK2_HUMAN	INHIBITOR	IC50	7.12		CHEMBL
Tyrosine-protein kinase JAK1	Kinase	P23458	JAK1_HUMAN	INHIBITOR	Ki	9.17		CHEMBL
G protein-coupled receptor kinase 7	Kinase	Q8WTQ7	GRK7_HUMAN		Kd	5.37		CHEMBL
Serine/threonine-protein kinase N2	Kinase	Q16513	PKN2_HUMAN		Kd	5.92		CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2	Kinase	Q5S007	LRRK2_HUMAN		Kd	6.26		CHEMBL
BMP-2-inducible protein kinase	Kinase	Q9NSY1	BMP2K_HUMAN		Kd	5.15		CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 2	Kinase	Q9HBH9	MKNK2_HUMAN		Kd	5.80		CHEMBL
Non-receptor tyrosine-protein kinase TYK2	Kinase	P29597	TYK2_HUMAN	INHIBITOR	Ki	8.36		CHEMBL
Calcium/calmodulin-dependent protein kinase type 1D	Kinase	Q8IU85	KCC1D_HUMAN		Kd	5.80		CHEMBL
Serine/threonine-protein kinase 3	Kinase	Q13188	STK3_HUMAN		Kd	5.37		CHEMBL
Tyrosine-protein kinase JAK3	Kinase	P52333	JAK3_HUMAN	INHIBITOR	IC50	8.48		WOMBAT-PK
Calcium/calmodulin-dependent protein kinase type II subunit alpha	Kinase	Q9UQM7	KCC2A_HUMAN		Kd	5.46		CHEMBL
Serine/threonine-protein kinase ULK3	Kinase	Q6PHR2	ULK3_HUMAN		Kd	5.19		CHEMBL
Rho-associated protein kinase 2	Kinase	O75116	ROCK2_HUMAN		Kd	6.38		CHEMBL
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN		Kd	5.96		CHEMBL
Protein kinase C delta type	Kinase	Q05655	KPCD_HUMAN		Kd	5.70		CHEMBL
Serine/threonine-protein kinase DCLK3	Kinase	Q9C098	DCLK3_HUMAN		Kd	8.35		CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN		Kd	5.48		CHEMBL
Myotonin-protein kinase	Kinase	Q09013	DMPK_HUMAN		Kd	5.92		CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		Kd	6.34		CHEMBL
NUAK family SNF1-like kinase 2	Kinase	Q9H093	NUAK2_HUMAN		Kd	6.62		CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta	Kinase	Q13557	KCC2D_HUMAN		Kd	5.57		CHEMBL
Serine/threonine-protein kinase N1	Kinase	Q16512	PKN1_HUMAN		Kd	6.77		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2	Kinase	Q12851	M4K2_HUMAN		Kd	5.32		CHEMBL
Non-receptor tyrosine-protein kinase TNK1	Kinase	Q13470	TNK1_HUMAN		Kd	6.92		CHEMBL
Ribosomal protein S6 kinase alpha-2	Kinase	Q15349	KS6A2_HUMAN		Kd	6.22		CHEMBL
Rho-associated protein kinase 1	Kinase	Q13464	ROCK1_HUMAN		Kd	6.33		CHEMBL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN		Kd	5.66		CHEMBL
Serine/threonine-protein kinase DCLK1	Kinase	O15075	DCLK1_HUMAN		Kd	5.17		CHEMBL
Serine/threonine-protein kinase PknB	Kinase		PKNB_MYCTU		Kd	5.70		CHEMBL
Tyrosine-protein kinase JAK3	Kinase		JAK3_MOUSE		IC50	7.32		CHEMBL
Tyrosine-protein kinase JAK2	Kinase		JAK2_MOUSE		IC50	5.69		CHEMBL

External reference:

ID	Source
D09783	KEGG_DRUG
4031786	VUID
N0000186059	NUI
C2930696	UMLSCUI
87LA6FU830	UNII
9298	INN_ID
CHEMBL221959	ChEMBL_ID
CHEMBL459769	ChEMBL_ID
540737-29-9	SECONDARY_CAS_RN
DB08895	DRUGBANK_ID
CHEBI:71200	CHEBI
C479163	MESH_SUPPLEMENTAL_RECORD_UI
CHEMBL2103743	ChEMBL_ID
9926791	PUBCHEM_CID
5677	IUPHAR_LIGAND_ID
704316006	SNOMEDCT_US
1357536	RXNORM
28976	MMSL
d07925	MMSL
014743	NDDF
4031786	VANDF
704313003	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
XELJANZ	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0501	TABLET, FILM COATED, EXTENDED RELEASE	11 mg	ORAL	NDA	20 sections
XELJANZ	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0502	TABLET, FILM COATED, EXTENDED RELEASE	22 mg	ORAL	NDA	20 sections
XELJANZ	HUMAN PRESCRIPTION DRUG LABEL	1	0069-1001	TABLET, FILM COATED	5 mg	ORAL	NDA	20 sections
XELJANZ	HUMAN PRESCRIPTION DRUG LABEL	1	0069-1002	TABLET, FILM COATED	10 mg	ORAL	NDA	20 sections
XELJANZ	HUMAN PRESCRIPTION DRUG LABEL	1	63539-012	TABLET, FILM COATED	5 mg	ORAL	NDA	20 sections
XELJANZ	HUMAN PRESCRIPTION DRUG LABEL	1	63539-016	TABLET, FILM COATED	10 mg	ORAL	NDA	20 sections
XELJANZ	HUMAN PRESCRIPTION DRUG LABEL	1	63539-501	TABLET, EXTENDED RELEASE	11 mg	ORAL	NDA	20 sections
XELJANZ	HUMAN PRESCRIPTION DRUG LABEL	1	63539-502	TABLET, EXTENDED RELEASE	22 mg	ORAL	NDA	20 sections