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

Stem definition	Drug id	CAS RN
proteasome inhibitors	4483	868540-17-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: carfilzomib kyprolis PR-171 PR 171	epoxomicin derivative proteasome inhibitor with antiproliferative and proapoptotic effects on primary human acute myeloid leukaemia cells Molecular weight: 719.92 Formula: C40H57N5O7 CLOGP: 4.21 LIPINSKI: 3 HAC: 12 HDO: 4 TPSA: 158.47 ALOGS: -5.17 ROTB: 20 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

carfilzomib
kyprolis
PR-171
PR 171

epoxomicin derivative proteasome inhibitor with antiproliferative and proapoptotic effects on primary human acute myeloid leukaemia cells

Molecular weight: 719.92
Formula: C40H57N5O7
CLOGP: 4.21
LIPINSKI: 3
HAC: 12
HDO: 4
TPSA: 158.47
ALOGS: -5.17
ROTB: 20

Status: OFP

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

Drug dosage:

None

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	0.13 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	39.50 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.10 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
July 20, 2012	FDA	ONYX PHARMS
July 4, 2016	PMDA	Ono Pharmaceutical

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
Intercepted product preparation error	390.01	18.45	78	17614	619	63470711
Thrombocytopenia	342.91	18.45	305	17387	150852	63320478
Plasma cell myeloma	308.15	18.45	165	17527	35740	63435590
Tumour lysis syndrome	189.42	18.45	77	17615	8913	63462417
Cytopenia	186.55	18.45	82	17610	11519	63459811
Death	178.47	18.45	349	17343	374032	63097298
Thrombotic microangiopathy	158.09	18.45	71	17621	10490	63460840
Neutropenia	155.02	18.45	216	17476	174789	63296541
Off label use	152.89	18.45	472	17220	673990	62797340
Platelet count decreased	151.63	18.45	174	17518	115948	63355382
Plasma cell myeloma recurrent	136.16	18.45	46	17646	3167	63468163
Plasma cell myeloma refractory	118.69	18.45	26	17666	333	63470997
Pneumonia	115.75	18.45	333	17359	456434	63014896
Unevaluable event	112.80	18.45	102	17590	51284	63420046
Neuropathy peripheral	110.68	18.45	147	17545	113520	63357810
Light chain analysis increased	106.55	18.45	31	17661	1302	63470028
Cardiac failure	105.36	18.45	127	17565	89015	63382315
Pancytopenia	104.75	18.45	132	17560	96801	63374529
Acute kidney injury	102.22	18.45	226	17466	263189	63208141
Pyrexia	101.31	18.45	324	17368	470154	63001176
Anaemia	84.08	18.45	224	17468	293206	63178124
Sepsis	79.06	18.45	148	17544	152975	63318355
Plasmacytoma	78.97	18.45	29	17663	2550	63468780
Therapy partial responder	74.94	18.45	43	17649	10615	63460715
Disease progression	70.13	18.45	124	17568	122634	63348696
Atypical haemolytic uraemic syndrome	67.29	18.45	19	17673	716	63470614
Body dysmorphic disorder	60.90	18.45	15	17677	329	63471001
Neutrophil count decreased	58.02	18.45	75	17617	56331	63414999
Febrile infection	57.06	18.45	20	17672	1537	63469793
Laboratory test abnormal	56.25	18.45	52	17640	26860	63444470
Drug hypersensitivity	55.16	18.45	10	17682	310677	63160653
Pulmonary embolism	53.12	18.45	107	17585	116577	63354753
Acute pulmonary oedema	52.29	18.45	31	17661	8127	63463203
White blood cell count decreased	51.19	18.45	117	17575	138987	63332343
Arthropathy	47.67	18.45	5	17687	234787	63236543
Plasma cell leukaemia	47.17	18.45	16	17676	1114	63470216
Leukopenia	46.61	18.45	80	17612	77210	63394120
Full blood count decreased	46.27	18.45	46	17646	25978	63445352
COVID-19	45.96	18.45	99	17593	113004	63358326
Arthralgia	45.76	18.45	55	17637	569655	62901675
Joint ankylosis	44.41	18.45	15	17677	1031	63470299
Joint swelling	44.23	18.45	18	17674	327648	63143682
Cerebellar haemangioma	43.30	18.45	9	17683	88	63471242
Condition aggravated	42.73	18.45	30	17662	402187	63069143
Protein total increased	42.60	18.45	19	17673	2758	63468572
Renal failure	42.22	18.45	98	17594	117554	63353776
Pneumococcal sepsis	41.79	18.45	13	17679	687	63470643
Alopecia	41.72	18.45	21	17671	337515	63133815
Product use issue	41.58	18.45	6	17686	220514	63250816
Lymphopenia	41.41	18.45	37	17655	18290	63453040
Musculoskeletal stiffness	39.99	18.45	3	17689	184615	63286715
Swelling	39.03	18.45	14	17678	275364	63195966
Cardiotoxicity	38.85	18.45	26	17666	8412	63462918
Glossodynia	38.48	18.45	3	17689	178873	63292457
Bone pain	37.56	18.45	60	17632	54581	63416749
COVID-19 pneumonia	36.77	18.45	31	17661	14178	63457152
Posterior reversible encephalopathy syndrome	35.25	18.45	33	17659	17312	63454018
Pulmonary oedema	34.67	18.45	58	17634	54815	63416515
Cerebral toxoplasmosis	33.70	18.45	12	17680	966	63470364
Dyspnoea	33.37	18.45	305	17387	661008	62810322
Fatigue	33.17	18.45	385	17307	887643	62583687
Pulmonary hypertension	33.02	18.45	46	17646	37077	63434253
Hypertensive crisis	32.84	18.45	30	17662	15256	63456074
Cardiac failure congestive	32.06	18.45	76	17616	92357	63378973
Wound	31.82	18.45	4	17688	163259	63308071
Abdominal discomfort	31.42	18.45	26	17666	320859	63150471
Respiratory failure	31.36	18.45	80	17612	101778	63369552
Pneumonia pneumococcal	30.32	18.45	14	17678	2201	63469129
Completed suicide	29.82	18.45	3	17689	145670	63325660
Pain	29.38	18.45	107	17585	740521	62730809
Asthenia	28.74	18.45	194	17498	383410	63087920
Hepatitis B reactivation	28.52	18.45	15	17677	3122	63468208
Drug ineffective	28.49	18.45	173	17519	1044592	62426738
Thrombotic thrombocytopenic purpura	28.37	18.45	16	17676	3820	63467510
Haemolytic anaemia	28.09	18.45	23	17669	10102	63461228
Light chain analysis abnormal	27.74	18.45	7	17685	170	63471160
Influenza	27.08	18.45	79	17613	108643	63362687
Treatment failure	26.73	18.45	11	17681	199032	63272298
Microangiopathic haemolytic anaemia	26.71	18.45	9	17683	614	63470716
Central nervous system vasculitis	26.54	18.45	10	17682	944	63470386
Polyneuropathy	26.32	18.45	26	17666	14563	63456767
Pericarditis	26.19	18.45	3	17689	131576	63339754
Cardiac disorder	26.02	18.45	49	17643	50767	63420563
Haemolytic uraemic syndrome	25.73	18.45	13	17679	2490	63468840
Osteolysis	24.04	18.45	13	17679	2861	63468469
Pneumonitis	23.28	18.45	38	17654	35184	63436146
Post procedural diarrhoea	23.22	18.45	8	17684	584	63470746
Drug interaction	23.12	18.45	18	17674	229113	63242217
Klebsiella sepsis	22.46	18.45	10	17682	1445	63469885
Anxiety disorder	22.39	18.45	14	17678	4036	63467294
Meningitis listeria	22.38	18.45	8	17684	651	63470679
Haemolysis	22.27	18.45	17	17675	6751	63464579
Acute respiratory distress syndrome	22.19	18.45	30	17662	23504	63447826
Febrile neutropenia	22.14	18.45	78	17614	118371	63352959
Bone lesion	22.10	18.45	16	17676	5865	63465465
Listeria sepsis	21.53	18.45	8	17684	727	63470603
Infusion site extravasation	21.50	18.45	20	17672	10406	63460924
Pneumonia bacterial	21.16	18.45	19	17673	9446	63461884
Aspergilloma	20.62	18.45	6	17686	252	63471078
Clostridial sepsis	20.28	18.45	7	17685	514	63470816
Meningitis pneumococcal	20.22	18.45	6	17686	270	63471060
Abdominal pain upper	19.85	18.45	17	17675	206427	63264903
Diarrhoea	19.83	18.45	294	17398	715072	62756258
Discomfort	19.79	18.45	11	17681	167363	63303967
Myeloma cast nephropathy	19.67	18.45	5	17687	125	63471205
Blister	19.42	18.45	6	17686	129808	63341522
Cryptosporidiosis infection	19.36	18.45	6	17686	313	63471017
Syncope	19.17	18.45	74	17618	117311	63354019
Cardiac failure acute	19.12	18.45	18	17674	9505	63461825
Occupational exposure to product	19.07	18.45	10	17682	2068	63469262
Migraine	19.03	18.45	3	17689	103343	63367987
Vertebral lesion	18.85	18.45	7	17685	635	63470695

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
Thrombocytopenia	287.08	18.00	408	20637	155839	34780047
Plasma cell myeloma	269.02	18.00	214	20831	41823	34894063
Intercepted product preparation error	240.40	18.00	91	20954	3987	34931899
Off label use	206.55	18.00	635	20410	418889	34516997
Thrombotic microangiopathy	184.26	18.00	101	20944	10529	34925357
Plasma cell myeloma recurrent	167.53	18.00	72	20973	4393	34931493
Pneumonia	157.15	18.00	526	20519	362101	34573785
Plasmacytoma	140.06	18.00	60	20985	3631	34932255
Plasma cell myeloma refractory	138.39	18.00	38	21007	577	34935309
Neuropathy peripheral	133.02	18.00	204	20841	83059	34852827
Unevaluable event	131.96	18.00	128	20917	32462	34903424
Cytopenia	127.37	18.00	85	20960	12638	34923248
Therapy partial responder	117.91	18.00	73	20972	9543	34926343
Neutropenia	102.62	18.00	264	20781	156514	34779372
Haemolytic uraemic syndrome	99.58	18.00	41	21004	2245	34933641
Drug interaction	97.73	18.00	11	21034	225935	34709951
Death	96.60	18.00	483	20562	397566	34538320
Platelet count decreased	94.76	18.00	217	20828	119500	34816386
Deep vein thrombosis	93.26	18.00	152	20893	65096	34870790
Fatigue	82.33	18.00	439	20606	370214	34565672
Disease progression	80.13	18.00	191	20854	107886	34828000
Tumour lysis syndrome	78.58	18.00	72	20973	16987	34918899
Cardiac failure	76.16	18.00	169	20876	91079	34844807
Plasma cell leukaemia	73.99	18.00	26	21019	918	34934968
Pyrexia	61.04	18.00	375	20670	332638	34603248
Light chain analysis increased	60.59	18.00	25	21020	1376	34934510
Influenza	53.19	18.00	102	20943	49564	34886322
Thrombotic thrombocytopenic purpura	52.86	18.00	30	21015	3340	34932546
Condition aggravated	52.60	18.00	25	21020	192171	34743715
COVID-19 pneumonia	47.86	18.00	55	20990	16912	34918974
Hypercalcaemia	46.79	18.00	52	20993	15416	34920470
Pancytopenia	45.27	18.00	143	20902	95014	34840872
Acute kidney injury	44.67	18.00	325	20720	304663	34631223
Infection	44.52	18.00	138	20907	90777	34845109
Bronchopneumopathy	43.59	18.00	15	21030	497	34935389
Atypical haemolytic uraemic syndrome	41.75	18.00	13	21032	312	34935574
Laboratory test abnormal	41.31	18.00	56	20989	20335	34915551
Ejection fraction decreased	40.95	18.00	54	20991	19100	34916786
COVID-19	37.29	18.00	117	20928	77433	34858453
Cardiac disorder	37.20	18.00	81	20964	43045	34892841
Infusion site pain	36.78	18.00	25	21020	3826	34932060
Infusion site extravasation	36.34	18.00	26	21019	4318	34931568
Dyspnoea	34.01	18.00	361	20684	376421	34559465
Sepsis	33.85	18.00	193	20852	166368	34769518
White blood cell count decreased	33.72	18.00	130	20915	95315	34840571
Atrial fibrillation	33.36	18.00	154	20891	122239	34813647
Progressive multifocal leukoencephalopathy	33.34	18.00	35	21010	9729	34926157
Anaemia	33.14	18.00	247	20798	233088	34702798
JC virus infection	32.87	18.00	19	21026	2189	34933697
Bone lesion	32.57	18.00	21	21024	2942	34932944
Cerebral toxoplasmosis	31.60	18.00	17	21028	1704	34934182
Pulmonary hypertension	31.56	18.00	50	20995	20874	34915012
Leukopenia	29.45	18.00	94	20951	62762	34873124
Cardiac failure acute	29.36	18.00	34	21011	10536	34925350
Pneumonia influenzal	27.80	18.00	15	21030	1513	34934373
Rhabdomyolysis	27.76	18.00	4	21041	68159	34867727
Rhinovirus infection	27.68	18.00	22	21023	4277	34931609
Pulmonary embolism	27.52	18.00	117	20928	89629	34846257
Atrial flutter	27.43	18.00	40	21005	15534	34920352
Blood immunoglobulin M increased	27.36	18.00	9	21036	259	34935627
Monoclonal immunoglobulin present	27.23	18.00	13	21032	1013	34934873
Protein total increased	27.11	18.00	17	21028	2270	34933616
Cardiac dysfunction	26.77	18.00	17	21028	2321	34933565
Haemolytic anaemia	26.29	18.00	32	21013	10447	34925439
Parainfluenzae virus infection	26.15	18.00	18	21027	2812	34933074
Abdominal pain	25.36	18.00	37	21008	163581	34772305
Morganella infection	24.92	18.00	10	21035	512	34935374
Infusion site erythema	24.72	18.00	16	21029	2257	34933629
Influenza A virus test positive	24.63	18.00	8	21037	221	34935665
Paraproteinaemia	24.52	18.00	9	21036	361	34935525
SARS-CoV-2 sepsis	24.43	18.00	7	21038	125	34935761
Osteolysis	24.42	18.00	18	21027	3130	34932756
Hypertensive crisis	24.05	18.00	28	21017	8723	34927163
Renal failure	23.74	18.00	147	20898	130410	34805476
Arthralgia	23.04	18.00	42	21003	169999	34765887
Bone pain	22.76	18.00	43	21002	20643	34915243
Monoclonal immunoglobulin increased	22.64	18.00	7	21038	164	34935722
Seizure	22.59	18.00	18	21027	104839	34831047
Brain natriuretic peptide increased	22.45	18.00	22	21023	5637	34930249
Pulmonary sepsis	22.34	18.00	15	21030	2250	34933636
Bronchial haemorrhage	21.97	18.00	10	21035	699	34935187
H1N1 influenza	21.97	18.00	11	21034	951	34934935
Salmonellosis	21.47	18.00	11	21034	998	34934888
Pathological fracture	21.12	18.00	19	21026	4372	34931514
Acute pulmonary oedema	21.03	18.00	24	21021	7319	34928567
Stress echocardiogram abnormal	20.95	18.00	4	21041	9	34935877
Infusion site swelling	20.87	18.00	15	21030	2509	34933377
Infusion site thrombosis	20.64	18.00	6	21039	113	34935773
Left ventricular failure	20.41	18.00	20	21025	5124	34930762
Microangiopathic haemolytic anaemia	19.57	18.00	10	21035	902	34934984
Pneumonia mycoplasmal	19.48	18.00	9	21036	651	34935235
Pruritus	19.29	18.00	35	21010	141946	34793940
Lymphopenia	19.28	18.00	35	21010	16300	34919586
Overdose	19.15	18.00	16	21029	91043	34844843
Phlebitis	19.12	18.00	17	21028	3853	34932033
Avian influenza	19.04	18.00	4	21041	17	34935869
Myelodysplastic syndrome	18.79	18.00	38	21007	19170	34916716
Myocardial necrosis marker increased	18.56	18.00	12	21033	1689	34934197
Vascular pain	18.53	18.00	6	21039	164	34935722
Respirovirus test positive	18.32	18.00	5	21040	74	34935812
Spinal pain	18.15	18.00	20	21025	5869	34930017
Left ventricular dysfunction	18.05	18.00	26	21019	9981	34925905

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
Intercepted product preparation error	515.19	16.54	144	33428	3416	79707400
Thrombocytopenia	502.16	16.54	587	32985	264672	79446144
Plasma cell myeloma	488.73	16.54	295	33277	52964	79657852
Cytopenia	308.26	16.54	157	33415	20226	79690590
Thrombotic microangiopathy	304.00	16.54	155	33417	20014	79690802
Pneumonia	276.78	16.54	751	32821	659495	79051321
Off label use	276.01	16.54	921	32651	906294	78804522
Death	269.66	16.54	676	32896	565838	79144978
Plasma cell myeloma recurrent	257.74	16.54	92	33480	4909	79705907
Unevaluable event	250.83	16.54	199	33373	55386	79655430
Tumour lysis syndrome	233.45	16.54	138	33434	23801	79687015
Platelet count decreased	232.45	16.54	344	33228	194320	79516496
Neutropenia	214.77	16.54	412	33160	287298	79423518
Plasmacytoma	200.76	16.54	74	33498	4329	79706487
Plasma cell myeloma refractory	193.62	16.54	47	33525	625	79710191
Disease progression	170.54	16.54	290	33282	184072	79526744
Light chain analysis increased	158.33	16.54	49	33523	1669	79709147
Neuropathy peripheral	156.14	16.54	241	33331	141064	79569752
Therapy partial responder	155.90	16.54	95	33477	17302	79693514
Pyrexia	148.49	16.54	621	32951	678088	79032728
Cardiac failure	146.38	16.54	246	33326	154596	79556220
Acute kidney injury	133.39	16.54	500	33072	518904	79191912
Sepsis	128.05	16.54	322	33250	269106	79441710
Pancytopenia	122.99	16.54	237	33335	165508	79545308
Anaemia	113.81	16.54	428	33144	444587	79266229
Deep vein thrombosis	104.89	16.54	185	33387	120734	79590082
Plasma cell leukaemia	104.04	16.54	36	33536	1750	79709066
Drug interaction	101.51	16.54	25	33547	415158	79295658
Haemolytic uraemic syndrome	96.79	16.54	44	33528	4405	79706411
COVID-19 pneumonia	90.67	16.54	84	33488	28765	79682051
Condition aggravated	87.94	16.54	51	33521	501073	79209743
Fatigue	87.70	16.54	679	32893	929048	78781768
Completed suicide	86.60	16.54	4	33568	245763	79465053
Thrombotic thrombocytopenic purpura	81.77	16.54	44	33528	6332	79704484
Atypical haemolytic uraemic syndrome	80.83	16.54	26	33546	1006	79709810
COVID-19	79.61	16.54	193	33379	157481	79553335
Pulmonary embolism	78.16	16.54	202	33370	171452	79539364
Protein total increased	68.67	16.54	33	33539	3746	79707070
White blood cell count decreased	67.39	16.54	203	33369	188085	79522731
Arthralgia	66.56	16.54	86	33486	571717	79139099
Drug hypersensitivity	65.64	16.54	22	33550	298894	79411922
Lymphopenia	63.20	16.54	71	33501	30486	79680330
Atrial fibrillation	63.12	16.54	205	33367	197681	79513135
Renal failure	59.48	16.54	203	33369	200765	79510051
Influenza	57.41	16.54	151	33421	129455	79581361
Acute pulmonary oedema	55.83	16.54	47	33525	14183	79696633
Laboratory test abnormal	52.66	16.54	62	33510	27986	79682830
Alopecia	52.60	16.54	16	33556	231339	79479477
Respiratory failure	52.01	16.54	181	33391	180730	79530086
Febrile infection	51.22	16.54	26	33546	3320	79707496
Joint swelling	49.68	16.54	30	33542	288616	79422200
Neutrophil count decreased	49.53	16.54	117	33455	93842	79616974
Pulmonary hypertension	47.51	16.54	78	33494	48002	79662814
Infusion site extravasation	47.29	16.54	37	33535	10071	79700745
Body dysmorphic disorder	46.34	16.54	13	33559	312	79710504
Hepatitis B reactivation	46.29	16.54	30	33542	6078	79704738
Bronchopneumopathy	46.25	16.54	16	33556	777	79710039
Cardiac failure acute	46.18	16.54	48	33524	18881	79691935
Ejection fraction decreased	45.37	16.54	64	33508	34513	79676303
Haemolytic anaemia	44.94	16.54	46	33526	17774	79693042
Atrial flutter	44.29	16.54	50	33522	21575	79689241
Septic shock	43.53	16.54	132	33440	122669	79588147
Bone pain	42.86	16.54	81	33491	55661	79655155
Posterior reversible encephalopathy syndrome	42.70	16.54	54	33518	26227	79684589
Microangiopathic haemolytic anaemia	42.63	16.54	18	33554	1509	79709307
Infection	41.92	16.54	207	33365	241505	79469311
Full blood count decreased	41.83	16.54	54	33518	26765	79684051
Musculoskeletal stiffness	41.82	16.54	11	33561	174997	79535819
Hypercalcaemia	41.61	16.54	65	33507	38365	79672451
Osteolysis	41.41	16.54	25	33547	4473	79706343
Abdominal pain	40.88	16.54	63	33509	389506	79321310
Arthropathy	40.70	16.54	12	33560	177099	79533717
Dyspnoea	40.69	16.54	544	33028	856481	78854335
Pulmonary oedema	40.27	16.54	104	33468	88150	79622666
Pneumonia influenzal	39.94	16.54	21	33551	2883	79707933
Bone lesion	39.84	16.54	27	33545	5892	79704924
Cerebellar haemangioma	39.60	16.54	9	33563	88	79710728
Febrile neutropenia	39.47	16.54	197	33375	230802	79480014
Cardiac failure congestive	37.94	16.54	139	33433	142263	79568553
Pruritus	35.78	16.54	70	33502	394578	79316238
Pathological fracture	35.68	16.54	32	33540	10505	79700311
Abdominal discomfort	35.44	16.54	32	33540	250695	79460121
Cerebral toxoplasmosis	35.13	16.54	18	33554	2344	79708472
Myeloma cast nephropathy	34.63	16.54	9	33563	160	79710656
Monoclonal immunoglobulin present	34.38	16.54	14	33558	1071	79709745
Brain natriuretic peptide increased	34.10	16.54	29	33543	8871	79701945
Swelling	33.94	16.54	25	33547	216686	79494130
Parainfluenzae virus infection	33.74	16.54	24	33548	5658	79705158
Cardiotoxicity	33.45	16.54	33	33539	12206	79698610
Infusion site pain	32.89	16.54	35	33537	14141	79696675
Pulmonary sepsis	32.55	16.54	20	33552	3692	79707124
Glossodynia	32.51	16.54	3	33569	103334	79607482
Light chain analysis abnormal	32.49	16.54	9	33563	206	79710610
Asthenia	32.21	16.54	343	33229	511346	79199470
SARS-CoV-2 sepsis	31.58	16.54	8	33564	128	79710688
Headache	30.88	16.54	156	33416	653616	79057200
Rhinovirus infection	30.65	16.54	26	33546	7927	79702889
Hyperviscosity syndrome	30.23	16.54	10	33562	423	79710393
Weight increased	29.91	16.54	44	33528	277342	79433474
Myelodysplastic syndrome	29.72	16.54	49	33523	30252	79680564
Overdose	29.16	16.54	21	33551	184185	79526631
Pain	28.84	16.54	176	33396	703626	79007190
Leukopenia	28.76	16.54	111	33461	116402	79594414
Left ventricular dysfunction	28.66	16.54	38	33534	19323	79691493
Wound	28.33	16.54	7	33565	116172	79594644
Injection site pain	27.71	16.54	10	33562	129828	79580988
Rhabdomyolysis	27.63	16.54	5	33567	103126	79607690
Renal disorder	27.33	16.54	57	33515	42048	79668768
Pneumonia bacterial	27.18	16.54	37	33535	19294	79691522
Respiratory tract infection	27.15	16.54	62	33510	48627	79662189
Product use issue	27.09	16.54	29	33543	209793	79501023
Hypertension	26.78	16.54	234	33338	330758	79380058
Hypertensive crisis	26.59	16.54	38	33534	20732	79690084
Impaired healing	26.39	16.54	3	33569	87652	79623164
Polyneuropathy	26.35	16.54	41	33531	24110	79686706
Hospitalisation	25.95	16.54	93	33479	94143	79616673
Blister	25.84	16.54	9	33563	119467	79591349
Cardiac dysfunction	25.84	16.54	18	33554	4106	79706710
Anxiety	25.28	16.54	41	33531	248471	79462345
Coma	24.66	16.54	6	33566	100643	79610173
Abdominal pain upper	24.62	16.54	35	33537	223784	79487032
Meningitis listeria	24.61	16.54	11	33561	1058	79709758
Sepsis syndrome	23.84	16.54	12	33560	1505	79709311
Contusion	23.50	16.54	17	33555	148759	79562057
Protein total abnormal	23.49	16.54	9	33563	586	79710230
Keratopathy	23.45	16.54	11	33561	1183	79709633
Hypogammaglobulinaemia	23.27	16.54	28	33544	12923	79697893
Depressed level of consciousness	23.22	16.54	6	33566	96646	79614170
Hepatic enzyme increased	22.73	16.54	26	33546	182584	79528232
Intentional product misuse	22.69	16.54	6	33566	95159	79615657
Cardiac disorder	22.65	16.54	70	33502	65687	79645129
Paraproteinaemia	22.49	16.54	8	33564	422	79710394
Dizziness	22.40	16.54	130	33442	526311	79184505
Stress echocardiogram abnormal	22.38	16.54	4	33568	9	79710807
Intercepted product administration error	22.38	16.54	8	33564	428	79710388
Joint ankylosis	22.38	16.54	13	33559	2167	79708649
Cardiomyopathy	22.35	16.54	42	33530	28732	79682084
Drug ineffective	22.31	16.54	321	33251	1080592	78630224
Salmonellosis	21.67	16.54	12	33560	1826	79708990
Weight decreased	21.51	16.54	77	33495	355121	79355695
Left ventricular failure	21.08	16.54	23	33549	9558	79701258
Platelet count abnormal	21.04	16.54	17	33555	4845	79705971
Morganella infection	20.96	16.54	10	33562	1117	79709699
Seizure	20.30	16.54	30	33542	188804	79522012
Feeling abnormal	19.98	16.54	125	33447	159074	79551742
Lactic acidosis	19.76	16.54	3	33569	70356	79640460
Vascular pain	19.75	16.54	9	33563	906	79709910
Bronchial haemorrhage	19.46	16.54	10	33562	1310	79709506
Embolic pneumonia	19.45	16.54	5	33567	85	79710731
Urticaria	19.35	16.54	30	33542	185171	79525645
Blood immunoglobulin A increased	19.13	16.54	9	33563	974	79709842
Discomfort	19.01	16.54	15	33557	125602	79585214
Post procedural diarrhoea	19.00	16.54	8	33564	666	79710150
Cardiac amyloidosis	18.96	16.54	11	33561	1829	79708987
Product use in unapproved indication	18.92	16.54	49	33523	250310	79460506
Central nervous system vasculitis	18.85	16.54	10	33562	1398	79709418
B precursor type acute leukaemia	18.80	16.54	7	33565	421	79710395
Influenza A virus test positive	18.67	16.54	8	33564	695	79710121
Blood cholesterol increased	18.64	16.54	6	33566	83714	79627102
Injection site erythema	18.51	16.54	5	33567	78192	79632624
Progressive multifocal leukoencephalopathy	18.46	16.54	32	33540	20568	79690248
Squamous cell carcinoma of skin	18.44	16.54	26	33546	14007	79696809
Treatment failure	18.41	16.54	27	33545	170459	79540357
Thrombosis	18.26	16.54	77	33495	84023	79626793
Panel-reactive antibody increased	18.24	16.54	3	33569	3	79710813
Tricuspid valve incompetence	18.16	16.54	31	33541	19681	79691135
Hospice care	18.03	16.54	22	33550	10302	79700514
Listeria sepsis	17.95	16.54	8	33564	764	79710052
Infusion site erythema	17.90	16.54	21	33551	9439	79701377
Spinal compression fracture	17.41	16.54	28	33544	16930	79693886
Alanine aminotransferase increased	17.30	16.54	26	33546	162544	79548272
Respiratory distress	17.29	16.54	59	33513	58280	79652536
Respirovirus test positive	17.16	16.54	5	33567	138	79710678
Acute respiratory distress syndrome	17.16	16.54	49	33523	44018	79666798
Hypervolaemia	17.14	16.54	48	33524	42642	79668174
Hypersensitivity	17.12	16.54	55	33517	262184	79448632
Hypoglycaemia	16.85	16.54	11	33561	101583	79609233
Dysphagia	16.76	16.54	16	33556	122120	79588696
Osteoarthritis	16.57	16.54	8	33564	87301	79623515

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01XG02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Proteasome inhibitors
FDA MoA	N0000175075	Proteasome Inhibitors
FDA EPC	N0000175604	Proteasome Inhibitor
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:52726	proteasome inhibitors

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

Disease	Relation	SNOMED_ID	DOID
Multiple myeloma	indication	109989006	DOID:9538
Relapse multiple myeloma	indication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.37	acidic
pKa2	5.23	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
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	7491704	April 14, 2025	KYPROLIS IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE OR MORE LINES OF THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	7491704	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DARATUMUMAB PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	7491704	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DEXAMETHASONE OR WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	8129346	April 14, 2025	KYPROLIS IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE OR MORE LINES OF THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	8129346	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DARATUMUMAB PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	8129346	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DEXAMETHASONE OR WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	8207127	April 14, 2025	KYPROLIS IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE OR MORE LINES OF THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	8207127	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DARATUMUMAB PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	8207127	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DEXAMETHASONE OR WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
30MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 3, 2016	RX	POWDER	INTRAVENOUS	7491704	April 14, 2025	KYPROLIS IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE OR MORE LINES OF THERAPY
30MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 3, 2016	RX	POWDER	INTRAVENOUS	7491704	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DARATUMUMAB PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
30MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 3, 2016	RX	POWDER	INTRAVENOUS	7491704	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DEXAMETHASONE OR WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
30MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 3, 2016	RX	POWDER	INTRAVENOUS	7491704	April 14, 2025	TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST TWO PRIOR THERAPIES INCLUDING BORTEZOMIB AND AN IMMUNOMODULATORY AGENT AND HAVE DEMONSTRATED DISEASE PROGRESSION ON OR WITHIN 60 DAYS OF COMPLETION OF THE LAST THERAPY
30MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 3, 2016	RX	POWDER	INTRAVENOUS	8129346	April 14, 2025	KYPROLIS IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE OR MORE LINES OF THERAPY
30MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 3, 2016	RX	POWDER	INTRAVENOUS	8129346	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DARATUMUMAB PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
30MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 3, 2016	RX	POWDER	INTRAVENOUS	8129346	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DEXAMETHASONE OR WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
30MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 3, 2016	RX	POWDER	INTRAVENOUS	8129346	April 14, 2025	TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST TWO PRIOR THERAPIES INCLUDING BORTEZOMIB AND AN IMMUNOMODULATORY AGENT AND HAVE DEMONSTRATED DISEASE PROGRESSION ON OR WITHIN 60 DAYS OF COMPLETION OF THE LAST THERAPY
30MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 3, 2016	RX	POWDER	INTRAVENOUS	8207127	April 14, 2025	KYPROLIS IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE OR MORE LINES OF THERAPY
30MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 3, 2016	RX	POWDER	INTRAVENOUS	8207127	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DARATUMUMAB PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
30MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 3, 2016	RX	POWDER	INTRAVENOUS	8207127	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DEXAMETHASONE OR WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
30MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 3, 2016	RX	POWDER	INTRAVENOUS	8207127	April 14, 2025	TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST TWO PRIOR THERAPIES INCLUDING BORTEZOMIB AND AN IMMUNOMODULATORY AGENT AND HAVE DEMONSTRATED DISEASE PROGRESSION ON OR WITHIN 60 DAYS OF COMPLETION OF THE LAST THERAPY
60MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	July 20, 2012	RX	POWDER	INTRAVENOUS	7491704	April 14, 2025	KYPROLIS IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE OR MORE LINES OF THERAPY
60MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	July 20, 2012	RX	POWDER	INTRAVENOUS	7491704	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DARATUMUMAB PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
60MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	July 20, 2012	RX	POWDER	INTRAVENOUS	7491704	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DEXAMETHASONE OR WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
60MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	July 20, 2012	RX	POWDER	INTRAVENOUS	7491704	April 14, 2025	TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST TWO PRIOR THERAPIES INCLUDING BORTEZOMIB AND AN IMMUNOMODULATORY AGENT AND HAVE DEMONSTRATED DISEASE PROGRESSION ON OR WITHIN 60 DAYS OF COMPLETION OF THE LAST THERAPY
60MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	July 20, 2012	RX	POWDER	INTRAVENOUS	8129346	April 14, 2025	KYPROLIS IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE OR MORE LINES OF THERAPY
60MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	July 20, 2012	RX	POWDER	INTRAVENOUS	8129346	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DARATUMUMAB PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
60MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	July 20, 2012	RX	POWDER	INTRAVENOUS	8129346	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DEXAMETHASONE OR WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
60MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	July 20, 2012	RX	POWDER	INTRAVENOUS	8129346	April 14, 2025	TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST TWO PRIOR THERAPIES INCLUDING BORTEZOMIB AND AN IMMUNOMODULATORY AGENT AND HAVE DEMONSTRATED DISEASE PROGRESSION ON OR WITHIN 60 DAYS OF COMPLETION OF THE LAST THERAPY
60MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	July 20, 2012	RX	POWDER	INTRAVENOUS	8207127	April 14, 2025	KYPROLIS IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE OR MORE LINES OF THERAPY
60MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	July 20, 2012	RX	POWDER	INTRAVENOUS	8207127	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DARATUMUMAB PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
60MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	July 20, 2012	RX	POWDER	INTRAVENOUS	8207127	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DEXAMETHASONE OR WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
60MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	July 20, 2012	RX	POWDER	INTRAVENOUS	8207127	April 14, 2025	TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST TWO PRIOR THERAPIES INCLUDING BORTEZOMIB AND AN IMMUNOMODULATORY AGENT AND HAVE DEMONSTRATED DISEASE PROGRESSION ON OR WITHIN 60 DAYS OF COMPLETION OF THE LAST THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	9511109	Oct. 21, 2029	KYPROLIS IS INDICATED IN COMBINATION WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	RE47954	Oct. 21, 2029	USE IN COMBINATION WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
30MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 3, 2016	RX	POWDER	INTRAVENOUS	9511109	Oct. 21, 2029	KYPROLIS IS INDICATED IN COMBINATION WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
30MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 3, 2016	RX	POWDER	INTRAVENOUS	RE47954	Oct. 21, 2029	USE IN COMBINATION WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
60MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	July 20, 2012	RX	POWDER	INTRAVENOUS	9511109	Oct. 21, 2029	KYPROLIS IS INDICATED IN COMBINATION WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
60MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	July 20, 2012	RX	POWDER	INTRAVENOUS	RE47954	Oct. 21, 2029	USE IN COMBINATION WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	Aug. 20, 2023	TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY IN COMBINATION WITH DARATUMUMAB AND DEXAMETHASONE
30MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 3, 2016	RX	POWDER	INTRAVENOUS	Aug. 20, 2023	TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY IN COMBINATION WITH DARATUMUMAB AND DEXAMETHASONE
60MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	July 20, 2012	RX	POWDER	INTRAVENOUS	Aug. 20, 2023	TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY IN COMBINATION WITH DARATUMUMAB AND DEXAMETHASONE

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	8.22	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Cathepsin B	Enzyme	P07858	CATB_HUMAN		IC50	4.96	CHEMBL
Proteasome subunit beta type-8	Enzyme	P28062	PSB8_HUMAN		IC50	7.85	CHEMBL
Proteasome subunit beta type-1	Enzyme	P20618	PSB1_HUMAN		IC50	5.84	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	4.04	CHEMBL
Glutathione S-transferase omega-1	Unclassified	P78417	GSTO1_HUMAN		IC50	6.82	CHEMBL
Proteasome subunit beta type-9	Enzyme	P28065	PSB9_HUMAN		IC50	5.62	CHEMBL
Proteasome subunit beta type-10	Enzyme	P40306	PSB10_HUMAN		IC50	6.21	CHEMBL
Proteasome subunit beta type-2	Enzyme	P49721	PSB2_HUMAN		IC50	6.69	CHEMBL

External reference:

ID	Source
72X6E3J5AR	UNII
D08880	KEGG_DRUG
4031662	VUID
N0000185509	NUI
4031662	VANDF
C2001856	UMLSCUI
CHEBI:65347	CHEBI
CHEMBL451887	ChEMBL_ID
11556711	PUBCHEM_CID
DB08889	DRUGBANK_ID
8859	INN_ID
C524865	MESH_SUPPLEMENTAL_RECORD_UI
7420	IUPHAR_LIGAND_ID
1302966	RXNORM
192152	MMSL
28679	MMSL
d07882	MMSL
014536	NDDF
713463006	SNOMEDCT_US
714783001	SNOMEDCT_US
3BV	PDB_CHEM_ID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
KYPROLIS	HUMAN PRESCRIPTION DRUG LABEL	1	76075-101	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	60 mg	INTRAVENOUS	NDA	31 sections
KYPROLIS	HUMAN PRESCRIPTION DRUG LABEL	1	76075-101	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	60 mg	INTRAVENOUS	NDA	31 sections
KYPROLIS	HUMAN PRESCRIPTION DRUG LABEL	1	76075-101	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	60 mg	INTRAVENOUS	NDA	31 sections
KYPROLIS	HUMAN PRESCRIPTION DRUG LABEL	1	76075-102	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	30 mg	INTRAVENOUS	NDA	31 sections
KYPROLIS	HUMAN PRESCRIPTION DRUG LABEL	1	76075-102	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	30 mg	INTRAVENOUS	NDA	31 sections
KYPROLIS	HUMAN PRESCRIPTION DRUG LABEL	1	76075-102	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	30 mg	INTRAVENOUS	NDA	31 sections
KYPROLIS	HUMAN PRESCRIPTION DRUG LABEL	1	76075-103	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	10 mg	INTRAVENOUS	NDA	31 sections
KYPROLIS	HUMAN PRESCRIPTION DRUG LABEL	1	76075-103	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	10 mg	INTRAVENOUS	NDA	31 sections
KYPROLIS	HUMAN PRESCRIPTION DRUG LABEL	1	76075-103	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	10 mg	INTRAVENOUS	NDA	31 sections