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

Stem definition	Drug id	CAS RN
proteasome inhibitors	5067	1072833-77-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ixazomib ixazomib citrate MLN2238 MLN9708 ninlaro	an oral proteasome inhibitor with antineoplastic activity; MLN2238 is the biologically active form of MLN9708 Molecular weight: 361.03 Formula: C14H19BCl2N2O4 CLOGP: 1.10 LIPINSKI: 0 HAC: 6 HDO: 4 TPSA: 98.66 ALOGS: -4.47 ROTB: 7 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ixazomib
ixazomib citrate
MLN2238
MLN9708
ninlaro

an oral proteasome inhibitor with antineoplastic activity; MLN2238 is the biologically active form of MLN9708

Molecular weight: 361.03
Formula: C14H19BCl2N2O4
CLOGP: 1.10
LIPINSKI: 0
HAC: 6
HDO: 4
TPSA: 98.66
ALOGS: -4.47
ROTB: 7

Status: ONP

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

Drug dosage:

None

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	3.61 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.50 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	97 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company
Nov. 21, 2016	EMA	Takeda Pharma A/S
Nov. 20, 2015	FDA	MILLENNIUM PHARMS
March 30, 2017	PMDA	Takeda Pharmaceutical Company 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
Diarrhoea	888.10	20.69	1196	22376	714170	62751280
Neuropathy peripheral	622.95	20.69	434	23138	113233	63352217
Death	556.19	20.69	687	22885	373694	63091756
Thrombocytopenia	335.78	20.69	343	23229	150814	63314636
Platelet count decreased	291.95	20.69	282	23290	115840	63349610
Pneumonia	252.12	20.69	535	23037	456232	63009218
Adverse event	243.05	20.69	201	23371	67358	63398092
Off label use	234.65	20.69	661	22911	673801	62791649
Plasma cell myeloma recurrent	220.42	20.69	71	23501	3142	63462308
Product physical issue	200.98	20.69	74	23498	4906	63460544
Plasma cell myeloma	188.88	20.69	134	23438	35771	63429679
Constipation	183.84	20.69	312	23260	224631	63240819
No adverse event	180.56	20.69	138	23434	41267	63424183
Nausea	164.81	20.69	688	22884	853783	62611667
Product dose omission issue	133.92	20.69	279	23293	234034	63231416
White blood cell count decreased	132.54	20.69	207	23365	138897	63326553
Cytopenia	113.09	20.69	64	23508	11537	63453913
Full blood count decreased	109.61	20.69	85	23487	25939	63439511
Laboratory test abnormal	96.52	20.69	80	23492	26832	63438618
Vomiting	96.05	20.69	436	23136	559181	62906269
Neutrophil count decreased	93.57	20.69	110	23462	56296	63409154
Neutropenia	75.97	20.69	187	23385	174818	63290632
Fatigue	64.83	20.69	555	23017	887473	62577977
Drug ineffective	63.86	20.69	189	23383	1044576	62420874
Dehydration	59.72	20.69	170	23402	173184	63292266
Condition aggravated	59.59	20.69	38	23534	402179	63063271
Light chain analysis increased	58.21	20.69	21	23551	1312	63464138
Infusion related reaction	54.96	20.69	12	23560	245509	63219941
Accidental exposure to product	54.93	20.69	59	23513	27346	63438104
Glossodynia	54.21	20.69	3	23569	178873	63286577
Influenza	52.34	20.69	121	23451	108601	63356849
Plasmacytoma	51.08	20.69	23	23549	2556	63462894
Monoclonal immunoglobulin present	51.07	20.69	17	23555	834	63464616
Treatment failure	50.50	20.69	7	23565	199036	63266414
Muscle spasms	49.80	20.69	149	23423	156001	63309449
Adverse drug reaction	49.03	20.69	98	23474	79616	63385834
Therapeutic product effect decreased	48.53	20.69	7	23565	193180	63272270
Drug interaction	47.76	20.69	13	23559	229118	63236332
Product packaging quantity issue	46.85	20.69	18	23554	1341	63464109
Wound	45.81	20.69	4	23568	163259	63302191
Hepatic enzyme increased	45.05	20.69	10	23562	202318	63263132
Asthenia	44.83	20.69	269	23303	383335	63082115
N-terminal prohormone brain natriuretic peptide decreased	44.63	20.69	8	23564	22	63465428
Cataract	43.63	20.69	77	23495	56976	63408474
Rash	43.07	20.69	355	23217	560516	62904934
COVID-19	42.96	20.69	115	23457	112988	63352462
Body dysmorphic disorder	42.65	20.69	12	23560	332	63465118
Back pain	42.26	20.69	202	23370	263943	63201507
Discomfort	42.18	20.69	6	23566	167368	63298082
Arthralgia	41.58	20.69	94	23478	569616	62895834
Musculoskeletal stiffness	39.37	20.69	10	23562	184608	63280842
Paraesthesia	38.51	20.69	137	23435	156829	63308621
Product use in unapproved indication	37.61	20.69	10	23562	179070	63286380
Drug hypersensitivity	37.56	20.69	36	23536	310651	63154799
Pain	37.55	20.69	145	23427	740483	62724967
Injection site pain	36.91	20.69	3	23569	129797	63335653
Cardiac amyloidosis	36.08	20.69	13	23559	809	63464641
Peripheral swelling	35.96	20.69	194	23378	265748	63199702
Product packaging issue	34.65	20.69	14	23558	1192	63464258
Toxicity to various agents	34.38	20.69	25	23547	247225	63218225
Product blister packaging issue	33.16	20.69	9	23563	217	63465233
Vitiligo	32.74	20.69	14	23558	1375	63464075
Monoclonal immunoglobulin increased	32.01	20.69	8	23564	138	63465312
Dry skin	30.36	20.69	66	23506	56821	63408629
Joint ankylosis	29.56	20.69	12	23560	1034	63464416
Anaemia	29.41	20.69	198	23374	293232	63172218
COVID-19 pneumonia	29.19	20.69	31	23541	14178	63451272
Blood potassium decreased	28.68	20.69	54	23518	41972	63423478
Ageusia	28.29	20.69	30	23542	13698	63451752
Hypertension	27.64	20.69	38	23534	279265	63186185
Arthropathy	27.45	20.69	28	23544	234764	63230686
Decreased appetite	27.34	20.69	173	23399	250879	63214571
Taste disorder	26.65	20.69	29	23543	13633	63451817
Illness	26.27	20.69	57	23515	49002	63416448
VIth nerve paresis	25.52	20.69	6	23566	79	63465371
Wheezing	25.10	20.69	3	23569	95592	63369858
Impaired healing	25.08	20.69	4	23568	102538	63362912
Hypersensitivity	24.98	20.69	44	23528	292641	63172809
Myelosuppression	24.95	20.69	37	23535	23666	63441784
Haemorrhoidal haemorrhage	24.89	20.69	17	23555	4262	63461188
Headache	24.87	20.69	136	23436	633105	62832345
Hypokalaemia	24.08	20.69	89	23483	103715	63361735
Herpes zoster	23.76	20.69	76	23496	82386	63383064
Hypoglossal nerve paresis	23.51	20.69	6	23566	113	63465337
Mobility decreased	23.20	20.69	8	23564	121151	63344299
Neutrophil count abnormal	23.03	20.69	14	23558	2878	63462572
Cardiac failure	22.87	20.69	79	23493	89063	63376387
Alopecia	22.73	20.69	58	23514	337478	63127972
Blood immunoglobulin G increased	22.60	20.69	13	23559	2414	63463036
Hypotension	22.35	20.69	42	23530	272562	63192888
Joint swelling	22.30	20.69	56	23516	327610	63137840
Eye swelling	21.90	20.69	35	23537	23883	63441567
Brain abscess	21.49	20.69	12	23560	2106	63463344
Bone pain	21.18	20.69	56	23516	54585	63410865
Protein total increased	20.98	20.69	13	23559	2764	63462686
Tumour lysis syndrome	20.97	20.69	21	23551	8969	63456481

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
Death	519.40	20.13	905	21045	397144	34537837
Neuropathy peripheral	514.71	20.13	422	21528	82841	34852140
Pneumonia	321.30	20.13	702	21248	361925	34573056
Diarrhoea	305.62	20.13	719	21231	389193	34545788
Adverse event	281.89	20.13	165	21785	18712	34916269
Off label use	271.19	20.13	719	21231	418805	34516176
Platelet count decreased	223.01	20.13	322	21628	119395	34815586
Plasma cell myeloma recurrent	221.71	20.13	89	21861	4376	34930605
No adverse event	221.08	20.13	152	21798	22775	34912206
Product physical issue	211.64	20.13	74	21876	2467	34932514
Thrombocytopenia	205.07	20.13	358	21592	155889	34779092
Plasma cell myeloma	171.64	20.13	169	21781	41868	34893113
Full blood count decreased	165.16	20.13	116	21834	17972	34917009
Light chain analysis increased	129.07	20.13	44	21906	1357	34933624
Fatigue	123.02	20.13	508	21442	370145	34564836
Drug interaction	120.58	20.13	5	21945	225941	34709040
Laboratory test abnormal	114.42	20.13	98	21852	20293	34914688
Product dose omission issue	114.41	20.13	240	21710	119471	34815510
Constipation	112.09	20.13	258	21692	136724	34798257
Rash	108.23	20.13	346	21604	222406	34712575
White blood cell count decreased	100.20	20.13	199	21751	95246	34839735
Peripheral swelling	90.64	20.13	168	21782	76373	34858608
Adverse drug reaction	87.73	20.13	100	21850	29242	34905739
COVID-19	81.72	20.13	162	21788	77388	34857593
Influenza	81.33	20.13	126	21824	49540	34885441
Accidental exposure to product	72.76	20.13	62	21888	12740	34922241
Back pain	64.33	20.13	195	21755	121594	34813387
Toxicity to various agents	60.65	20.13	25	21925	200337	34734644
Lower respiratory tract infection	55.64	20.13	83	21867	31554	34903427
Cytopenia	53.44	20.13	52	21898	12671	34922310
Respiratory tract infection viral	48.40	20.13	26	21924	2491	34932490
Respiratory tract infection bacterial	47.66	20.13	23	21927	1759	34933222
Product use in unapproved indication	45.94	20.13	9	21941	117490	34817491
Condition aggravated	43.78	20.13	34	21916	192162	34742819
Product packaging issue	43.02	20.13	16	21934	638	34934343
Respiratory tract infection	39.45	20.13	55	21895	19657	34915324
Monoclonal immunoglobulin present	39.29	20.13	17	21933	1009	34933972
Neutrophil count abnormal	37.57	20.13	20	21930	1882	34933099
Neutropenia	36.94	20.13	195	21755	156583	34778398
Tachycardia	36.46	20.13	5	21945	84767	34850214
Muscle spasms	35.77	20.13	116	21834	74885	34860096
Hypertension	35.24	20.13	21	21929	136422	34798559
Full blood count increased	35.04	20.13	15	21935	867	34934114
Product blister packaging issue	34.66	20.13	9	21941	104	34934877
Product packaging quantity issue	34.29	20.13	15	21935	914	34934067
Thrombosis	33.65	20.13	88	21862	50370	34884611
Nausea	32.59	20.13	341	21609	339567	34595414
Keratopathy	32.50	20.13	13	21937	632	34934349
Rhabdomyolysis	31.86	20.13	3	21947	68160	34866821
Nasopharyngitis	31.38	20.13	106	21844	69862	34865119
Illness	30.49	20.13	40	21910	13489	34921492
Morganella infection	27.98	20.13	11	21939	511	34934470
Hypotension	27.18	20.13	62	21888	221587	34713394
Abdominal pain	27.04	20.13	38	21912	163580	34771401
Protein total increased	26.45	20.13	17	21933	2270	34932711
Malaise	26.27	20.13	203	21747	185622	34749359
Cryptosporidiosis infection	25.20	20.13	10	21940	476	34934505
Asthenia	24.85	20.13	249	21701	245002	34689979
Bronchial haemorrhage	24.73	20.13	11	21939	698	34934283
JC virus CSF test positive	24.51	20.13	7	21943	118	34934863
Insomnia	24.27	20.13	129	21821	103778	34831203
Paraproteinaemia	24.15	20.13	9	21941	361	34934620
Laryngeal cancer metastatic	23.98	20.13	6	21944	59	34934922
Light chain disease	23.93	20.13	7	21943	129	34934852
Bradycardia	23.45	20.13	9	21941	75409	34859572
Seizure	23.28	20.13	19	21931	104838	34830143
Plasma cell myeloma refractory	22.93	20.13	10	21940	605	34934376
Spinal pain	22.75	20.13	23	21927	5866	34929115
Chillblains	22.61	20.13	5	21945	27	34934954
Clonal haematopoiesis	22.46	20.13	6	21944	78	34934903
Overdose	22.15	20.13	15	21935	91044	34843937
Cataract	22.08	20.13	50	21900	26136	34908845
Hypoglycaemia	21.73	20.13	4	21946	54636	34880345
Plasmacytoma	21.22	20.13	18	21932	3673	34931308
Otitis externa bacterial	21.11	20.13	4	21946	8	34934973
Unevaluable event	20.87	20.13	56	21894	32534	34902447
Immunoglobulins decreased	20.82	20.13	10	21940	757	34934224
Cellulitis enterococcal	20.70	20.13	6	21944	107	34934874

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
Neuropathy peripheral	737.37	19.14	517	28137	140788	79574946
Diarrhoea	705.64	19.14	1182	27472	879307	78836427
Pneumonia	550.45	19.14	904	27750	659342	79056392
Off label use	507.53	19.14	1045	27609	906170	78809564
Platelet count decreased	448.95	19.14	444	28210	194220	79521514
Thrombocytopenia	430.26	19.14	502	28152	264757	79450977
Death	335.58	19.14	670	27984	565844	79149890
Plasma cell myeloma recurrent	299.86	19.14	99	28555	4902	79710832
Plasma cell myeloma	247.53	19.14	182	28472	53077	79662657
Product physical issue	219.81	19.14	75	28579	4110	79711624
No adverse event	200.17	19.14	139	28515	37053	79678681
Product dose omission issue	174.45	19.14	316	28338	247221	79468513
White blood cell count decreased	162.40	19.14	263	28391	188025	79527709
Constipation	149.34	19.14	320	28334	282730	79433004
Neutrophil count decreased	130.86	19.14	165	28489	93794	79621940
Full blood count decreased	120.83	19.14	90	28564	26729	79689005
Rash	117.67	19.14	464	28190	577894	79137840
Light chain analysis increased	115.09	19.14	37	28617	1681	79714053
COVID-19	103.01	19.14	195	28459	157479	79558255
Drug interaction	102.38	19.14	14	28640	415169	79300565
Nausea	88.84	19.14	617	28037	956579	78759155
Influenza	85.51	19.14	161	28493	129445	79586289
Cytopenia	79.95	19.14	63	28591	20320	79695414
Fatigue	77.37	19.14	584	28070	929143	78786591
Neutropenia	72.75	19.14	248	28406	287462	79428272
Laboratory test abnormal	64.43	19.14	64	28590	27984	79687750
Toxicity to various agents	62.55	19.14	37	28617	421503	79294231
Respiratory tract infection	57.66	19.14	79	28575	48610	79667124
Respiratory tract infection bacterial	56.60	19.14	23	28631	2054	79713680
Plasmacytoma	54.05	19.14	28	28626	4375	79711359
Condition aggravated	53.29	19.14	61	28593	501063	79214671
Accidental exposure to product	50.04	19.14	59	28595	31263	79684471
Pain	50.02	19.14	112	28542	703690	79012044
Anaemia	49.65	19.14	301	28353	444714	79271020
Neutrophil count abnormal	47.87	19.14	24	28630	3502	79712232
Product blister packaging issue	47.82	19.14	12	28642	218	79715516
Product packaging quantity issue	47.55	19.14	18	28636	1331	79714403
COVID-19 pneumonia	47.18	19.14	55	28599	28794	79686940
Dehydration	46.93	19.14	195	28459	247992	79467742
Product use in unapproved indication	46.43	19.14	16	28638	250343	79465391
Respiratory tract infection viral	46.37	19.14	25	28629	4234	79711500
Hypertension	45.06	19.14	32	28622	330960	79384774
Back pain	44.83	19.14	222	28432	303958	79411776
Myelosuppression	44.16	19.14	63	28591	40233	79675501
Musculoskeletal stiffness	42.84	19.14	6	28648	175002	79540732
Drug ineffective	42.71	19.14	222	28432	1080691	78635043
Drug hypersensitivity	41.87	19.14	28	28626	298888	79416846
Vomiting	41.21	19.14	392	28262	665436	79050298
Treatment failure	39.13	19.14	7	28647	170479	79545255
Body dysmorphic disorder	39.12	19.14	11	28643	314	79715420
Plasma cell myeloma refractory	39.06	19.14	13	28641	659	79715075
Cardiac amyloidosis	38.86	19.14	17	28637	1823	79713911
Keratopathy	38.75	19.14	15	28639	1179	79714555
Infusion related reaction	37.35	19.14	18	28636	230219	79485515
Peripheral swelling	37.06	19.14	193	28461	269424	79446310
Therapeutic product effect decreased	37.02	19.14	7	28647	163856	79551878
Monoclonal immunoglobulin present	36.53	19.14	14	28640	1071	79714663
N-terminal prohormone brain natriuretic peptide decreased	36.51	19.14	7	28647	32	79715702
Hypotension	36.45	19.14	64	28590	440253	79275481
Cataract	35.87	19.14	73	28581	62047	79653687
Injection site pain	35.46	19.14	3	28651	129835	79585899
Cardiac failure	35.21	19.14	129	28525	154713	79561021
Arthralgia	35.12	19.14	98	28556	571705	79144029
Product packaging issue	34.79	19.14	14	28640	1219	79714515
Headache	34.54	19.14	120	28534	653652	79062082
Taste disorder	34.31	19.14	35	28619	15788	79699946
Arthropathy	33.38	19.14	11	28643	177100	79538634
Hepatic enzyme increased	33.28	19.14	12	28642	182598	79533136
Polyneuropathy	29.82	19.14	40	28614	24111	79691623
Muscle spasms	29.71	19.14	133	28521	174597	79541137
Full blood count increased	29.18	19.14	10	28644	555	79715179
Discomfort	29.16	19.14	5	28649	125612	79590122
Herpes zoster	28.71	19.14	86	28568	92997	79622737
Hypokalaemia	27.84	19.14	114	28540	143926	79571808
Vitiligo	27.59	19.14	14	28640	2095	79713639
Sepsis	27.33	19.14	178	28476	269250	79446484
Tachycardia	27.18	19.14	15	28639	177753	79537981
Monoclonal immunoglobulin increased	26.85	19.14	7	28647	149	79715585
COVID-19 immunisation	26.58	19.14	12	28642	1387	79714347
Cryptosporidiosis infection	26.50	19.14	10	28644	733	79715001
Pneumonia influenzal	26.03	19.14	15	28639	2889	79712845
JC virus CSF test positive	26.01	19.14	7	28647	169	79715565
Mobility decreased	25.98	19.14	6	28648	122169	79593565
Blood immunoglobulin G increased	25.63	19.14	15	28639	2974	79712760
Nasopharyngitis	25.30	19.14	167	28487	253714	79462020
Asthenia	24.85	19.14	287	28367	511402	79204332
Bone lesion	24.74	19.14	19	28635	5900	79709834
Alopecia	24.71	19.14	28	28626	231327	79484407
Blood pressure increased	24.35	19.14	24	28630	211336	79504398
Glossodynia	24.24	19.14	4	28650	103333	79612401
Light chain disease	24.16	19.14	7	28647	223	79715511
Upper respiratory tract inflammation	23.87	19.14	16	28638	4019	79711715
Blood calcium abnormal	23.52	19.14	11	28643	1378	79714356
Overdose	23.52	19.14	19	28635	184187	79531547
Platelet count abnormal	23.43	19.14	17	28637	4845	79710889
Hypoglossal nerve paresis	23.41	19.14	6	28648	119	79715615
Hypercalcaemia	23.18	19.14	46	28608	38384	79677350
Rash macular	23.01	19.14	39	28615	28860	79686874
Hypersensitivity	22.70	19.14	37	28617	262202	79453532
Laryngeal cancer metastatic	22.69	19.14	5	28649	50	79715684
VIth nerve paresis	22.53	19.14	6	28648	139	79715595
Morganella infection	22.47	19.14	10	28644	1117	79714617
Wheezing	22.41	19.14	7	28647	116657	79599077
Immunoglobulins decreased	22.31	19.14	11	28643	1549	79714185
Adverse drug reaction	22.06	19.14	63	28591	66329	79649405
Hypoaesthesia	21.66	19.14	124	28530	179228	79536506
Intentional product misuse	21.63	19.14	4	28650	95161	79620573
Renal failure	21.12	19.14	134	28520	200834	79514900
Bronchial haemorrhage	20.96	19.14	10	28644	1310	79714424
Arnold-Chiari malformation	20.53	19.14	6	28648	197	79715537
Light chain analysis abnormal	20.19	19.14	6	28648	209	79715525
Squamous cell carcinoma of skin	20.07	19.14	25	28629	14008	79701726
Protein total increased	20.03	19.14	14	28640	3765	79711969
Bradycardia	19.92	19.14	12	28642	135545	79580189
Upper respiratory tract infection	19.91	19.14	75	28579	91093	79624641
Peripheral sensory neuropathy	19.91	19.14	24	28630	13009	79702725
Oxygen saturation decreased	19.57	19.14	11	28643	129036	79586698
Coma	19.40	19.14	6	28648	100643	79615091
Phyllodes tumour	19.30	19.14	4	28650	29	79715705
Migraine	19.20	19.14	4	28650	87489	79628245

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01XG03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Proteasome inhibitors
FDA MoA	N0000175075	Proteasome Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D011480	Protease Inhibitors
FDA EPC	N0000175604	Proteasome Inhibitor
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:50266	Prodrugs
CHEBI has role	CHEBI:52726	proteasome inhibitors
CHEBI has role	CHEBI:68495	Type I cell-death inducers
CHEBI has role	CHEBI:71031	orphan drugs
CHEBI has role	CHEBI:49103	drug metabolites

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

Disease	Relation	SNOMED_ID	DOID
Multiple myeloma	indication	109989006	DOID:9538

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.27	acidic
pKa2	12.17	acidic
pKa3	13.45	acidic

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 2.3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	9233115	Aug. 12, 2024	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	9233115	Aug. 12, 2024	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 4MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	9233115	Aug. 12, 2024	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 2.3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	8003819	Aug. 6, 2027	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 2.3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	8530694	Aug. 6, 2027	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 2.3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	8871745	Aug. 6, 2027	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	8003819	Aug. 6, 2027	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	8530694	Aug. 6, 2027	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	8871745	Aug. 6, 2027	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 4MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	8003819	Aug. 6, 2027	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 4MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	8530694	Aug. 6, 2027	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 4MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	8871745	Aug. 6, 2027	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 2.3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	9175017	June 16, 2029	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	9175017	June 16, 2029	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 4MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	9175017	June 16, 2029	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 2.3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	7442830	Nov. 20, 2029	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	7442830	Nov. 20, 2029	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 4MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	7442830	Nov. 20, 2029	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Proteasome subunit beta type-5	Enzyme	P28074	PSB5_HUMAN	INHIBITOR	IC50	8.47	SCIENTIFIC LITERATURE	DRUG LABEL
Proteasome subunit beta type-1	Enzyme	P20618	PSB1_HUMAN	INHIBITOR	IC50	7.51	SCIENTIFIC LITERATURE
Proteasome subunit beta type-2	Enzyme	P49721	PSB2_HUMAN	INHIBITOR	IC50	5.46	SCIENTIFIC LITERATURE
ATP-dependent Clp protease proteolytic subunit	Enzyme		CLPP_STAA8		EC50	5.44	CHEMBL
NACHT, LRR and PYD domains-containing protein 3	Unclassified		NLRP3_MOUSE		IC50	6.70	CHEMBL

External reference:

ID	Source
71050168A2	UNII
D10130	KEGG_DRUG
1239908-20-3	SECONDARY_CAS_RN
4035138	VANDF
C3273711	UMLSCUI
CHEBI:90942	CHEBI
6V8	PDB_CHEM_ID
CHEMBL2141296	ChEMBL_ID
25183872	PUBCHEM_CID
DB09570	DRUGBANK_ID
CHEMBL3545432	ChEMBL_ID
CHEMBL1813256	ChEMBL_ID
9411	INN_ID
C548400	MESH_SUPPLEMENTAL_RECORD_UI
C000595706	MESH_SUPPLEMENTAL_RECORD_UI
8450	IUPHAR_LIGAND_ID
1723734	RXNORM
237159	MMSL
31293	MMSL
d08398	MMSL
016599	NDDF
016600	NDDF
715256005	SNOMEDCT_US
781324002	SNOMEDCT_US
784168005	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-078	CAPSULE	2.30 mg	ORAL	NDA	29 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-078	CAPSULE	2.30 mg	ORAL	NDA	29 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-079	CAPSULE	3 mg	ORAL	NDA	29 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-079	CAPSULE	3 mg	ORAL	NDA	29 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-080	CAPSULE	4 mg	ORAL	NDA	29 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-080	CAPSULE	4 mg	ORAL	NDA	29 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-230	CAPSULE	2.30 mg	ORAL	NDA	33 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-230	CAPSULE	2.30 mg	ORAL	NDA	33 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-230	CAPSULE	2.30 mg	ORAL	NDA	33 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-390	CAPSULE	3 mg	ORAL	NDA	33 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-390	CAPSULE	3 mg	ORAL	NDA	33 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-390	CAPSULE	3 mg	ORAL	NDA	33 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-400	CAPSULE	4 mg	ORAL	NDA	33 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-400	CAPSULE	4 mg	ORAL	NDA	33 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-400	CAPSULE	4 mg	ORAL	NDA	33 sections