All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Stem definition	Drug id	CAS RN
antineoplastic, alkylating agents, methanesulfonates	438	55-98-1

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: busilvex busulfan busulfex busulphan citosulfan glyzophrol leucosulfan sulphabutin

An alkylating agent having a selective immunosuppressive effect on BONE MARROW. It has been used in the palliative treatment of chronic myeloid leukemia (MYELOID LEUKEMIA, CHRONIC), but although symptomatic relief is provided, no permanent remission is brought about. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), busulfan is listed as a known carcinogen. Molecular weight: 246.29 Formula: C6H14O6S2 CLOGP: -0.59 LIPINSKI: 0 HAC: 6 HDO: 0 TPSA: 86.74 ALOGS: -1.68 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

None

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.10 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	1 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.23 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	70 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.55 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	2.40 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	1 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	3.40 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
June 26, 1954	FDA	ASPEN GLOBAL
March 25, 2020	PMDA	Otsuka Pharmaceutical Co., Ltd

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
Acute graft versus host disease	1005.88	34.56	228	13670	3947	56274222
Graft versus host disease	812.77	34.56	211	13687	6570	56271599
Chronic graft versus host disease	806.85	34.56	182	13716	3074	56275095
Cytomegalovirus infection	758.99	34.56	253	13645	19043	56259126
Venoocclusive liver disease	650.03	34.56	162	13736	4259	56273910
Acute graft versus host disease in skin	638.45	34.56	150	13748	3052	56275117
Product use in unapproved indication	503.63	34.56	353	13545	140469	56137700
Graft versus host disease in skin	473.00	34.56	114	13784	2593	56275576
Venoocclusive disease	465.24	34.56	106	13792	1871	56276298
Mucosal inflammation	394.04	34.56	198	13700	42612	56235557
Cytomegalovirus viraemia	382.97	34.56	110	13788	5010	56273159
Graft versus host disease in gastrointestinal tract	349.70	34.56	91	13807	2848	56275321
Cystitis haemorrhagic	341.61	34.56	95	13803	3842	56274327
Ovarian failure	340.24	34.56	75	13823	1130	56277039
Acute graft versus host disease in intestine	298.61	34.56	72	13826	1638	56276531
Thrombotic microangiopathy	245.38	34.56	91	13807	9320	56268849
Acute myeloid leukaemia recurrent	219.51	34.56	55	13843	1473	56276696
Premature menopause	210.00	34.56	47	13851	761	56277408
Transplant failure	205.28	34.56	52	13846	1457	56276712
Adenovirus infection	192.73	34.56	59	13839	3349	56274820
Febrile neutropenia	190.91	34.56	178	13720	105367	56172802
Viral haemorrhagic cystitis	189.01	34.56	43	13855	752	56277417
Cytomegalovirus infection reactivation	183.93	34.56	56	13842	3120	56275049
Primary hypogonadism	180.45	34.56	32	13866	138	56278031
Ovarian atrophy	177.53	34.56	29	13869	66	56278103
Post transplant lymphoproliferative disorder	166.58	34.56	57	13841	4615	56273554
Epstein-Barr virus infection	154.45	34.56	61	13837	7402	56270767
BK virus infection	152.05	34.56	48	13850	3016	56275153
Posterior reversible encephalopathy syndrome	141.30	34.56	72	13826	15888	56262281
Acute graft versus host disease in liver	136.54	34.56	32	13866	641	56277528
Bacteraemia	131.10	34.56	68	13830	15563	56262606
Blood follicle stimulating hormone increased	130.19	34.56	24	13874	134	56278035
Human herpesvirus 6 infection	128.88	34.56	41	13857	2641	56275528
Acute lymphocytic leukaemia recurrent	126.62	34.56	39	13859	2258	56275911
Blood luteinising hormone increased	125.58	34.56	22	13876	87	56278082
Chronic graft versus host disease in skin	123.65	34.56	30	13868	700	56277469
Idiopathic pneumonia syndrome	122.34	34.56	26	13872	326	56277843
Multiple organ dysfunction syndrome	119.15	34.56	101	13797	52669	56225500
Off label use	117.40	34.56	351	13547	555829	55722340
Cytomegalovirus chorioretinitis	107.18	34.56	32	13866	1666	56276503
Systemic mycosis	100.70	34.56	28	13870	1129	56277040
Acute myeloid leukaemia	98.70	34.56	58	13840	16914	56261255
Upper respiratory fungal infection	97.24	34.56	19	13879	151	56278018
Leukaemia recurrent	96.88	34.56	28	13870	1300	56276869
Mucormycosis	95.60	34.56	33	13865	2741	56275428
Pulmonary haemorrhage	95.06	34.56	42	13856	6741	56271428
Thrombocytopenia	90.85	34.56	138	13760	136086	56142083
Aplastic anaemia	90.00	34.56	44	13854	8884	56269285
Bacterial sepsis	89.49	34.56	34	13864	3715	56274454
Cystitis viral	88.17	34.56	17	13881	125	56278044
Cytomegalovirus test positive	87.34	34.56	31	13867	2795	56275374
Pain	86.95	34.56	28	13870	663156	55615013
Fatigue	78.86	34.56	49	13849	788503	55489666
Graft versus host disease in lung	77.65	34.56	18	13880	343	56277826
Arthralgia	77.62	34.56	15	13883	501654	55776515
Neurotoxicity	76.47	34.56	48	13850	15747	56262422
Alternaria infection	73.65	34.56	16	13882	224	56277945
Toxoplasmosis	72.93	34.56	23	13875	1439	56276730
Transplant dysfunction	71.74	34.56	31	13867	4715	56273454
Dizziness	70.70	34.56	6	13892	376134	55902035
Bronchopulmonary aspergillosis	69.42	34.56	36	13862	8228	56269941
Neutropenia	69.36	34.56	133	13765	158034	56120135
Disseminated mucormycosis	68.06	34.56	14	13884	148	56278021
Adenoviral hepatitis	67.59	34.56	16	13882	335	56277834
Headache	67.42	34.56	27	13871	559017	55719152
Bone marrow failure	65.57	34.56	55	13843	28231	56249938
Encephalitis cytomegalovirus	64.89	34.56	17	13881	545	56277624
Fall	63.76	34.56	7	13891	357503	55920666
Laryngitis fungal	63.50	34.56	13	13885	134	56278035
Nodular melanoma	61.55	34.56	11	13887	50	56278119
Neoplasm recurrence	61.17	34.56	23	13875	2441	56275728
JC virus infection	59.22	34.56	21	13877	1888	56276281
Haemophagocytic lymphohistiocytosis	59.05	34.56	34	13864	9538	56268631
Respiratory failure	57.32	34.56	92	13806	94970	56183199
Stem cell transplant	57.21	34.56	20	13878	1724	56276445
Epstein-Barr viraemia	55.92	34.56	17	13881	941	56277228
Aspergillus infection	55.57	34.56	30	13868	7435	56270734
Obliterative bronchiolitis	54.85	34.56	20	13878	1948	56276221
Pulmonary veno-occlusive disease	54.18	34.56	17	13881	1046	56277123
Bone marrow transplant rejection	53.92	34.56	10	13888	58	56278111
Drug hypersensitivity	52.76	34.56	4	13894	275201	56002968
Pancytopenia	52.31	34.56	85	13813	88630	56189539
Acute respiratory distress syndrome	51.58	34.56	43	13855	21883	56256286
Staphylococcal sepsis	50.46	34.56	28	13870	7321	56270848
Drug resistance	49.80	34.56	41	13857	20501	56257668
Citrobacter bacteraemia	49.67	34.56	8	13890	16	56278153
Recurrent cancer	48.81	34.56	18	13880	1810	56276359
Ascites	48.75	34.56	53	13845	37491	56240678
Hypersensitivity	48.39	34.56	4	13894	256404	56021765
Engraft failure	47.13	34.56	12	13886	343	56277826
Progressive multifocal leukoencephalopathy	47.11	34.56	32	13866	11981	56266188
Staphylococcal infection	46.93	34.56	52	13846	37566	56240603
Myelodysplastic syndrome	46.74	34.56	36	13862	16370	56261799
Hepatomegaly	46.53	34.56	31	13867	11244	56266925
Pyrexia	45.51	34.56	214	13684	418559	55859610
Myelosuppression	44.76	34.56	36	13862	17419	56260750
Human polyomavirus infection	44.23	34.56	11	13887	285	56277884
Back pain	43.93	34.56	4	13894	237166	56041003
Complications of bone marrow transplant	43.89	34.56	12	13886	454	56277715
Drug intolerance	42.86	34.56	7	13891	264811	56013358
Alopecia	42.79	34.56	10	13888	293448	55984721
Disseminated toxoplasmosis	42.11	34.56	9	13889	116	56278053
Device related infection	41.57	34.56	38	13860	21842	56256327
Hepatic necrosis	41.35	34.56	22	13876	5294	56272875
Streptococcal bacteraemia	40.83	34.56	15	13883	1492	56276677
Haematuria	40.20	34.56	41	13857	26946	56251223
Blood stem cell transplant failure	40.01	34.56	9	13889	149	56278020
Autoimmune haemolytic anaemia	39.90	34.56	20	13878	4256	56273913
Septic shock	39.59	34.56	61	13837	60774	56217395
Lower respiratory tract infection fungal	39.03	34.56	10	13888	293	56277876
Sepsis	38.91	34.56	98	13800	139742	56138427
Hypogonadism	38.44	34.56	8	13890	90	56278079
Arthropathy	38.12	34.56	3	13895	200272	56077897
Focal nodular hyperplasia	38.07	34.56	11	13887	510	56277659
Hilar lymphadenopathy	37.70	34.56	13	13885	1076	56277093
Pruritus	36.93	34.56	16	13882	316607	55961562
Dedifferentiated liposarcoma	36.36	34.56	7	13891	51	56278118
Bronchiolitis obliterans syndrome	36.18	34.56	8	13890	122	56278047
Fungaemia	35.84	34.56	15	13883	2109	56276060
Primary adrenal insufficiency	35.82	34.56	8	13890	128	56278041
Adrenal haemorrhage	35.36	34.56	10	13888	429	56277740
Candida sepsis	35.23	34.56	13	13885	1309	56276860
Bone marrow transplant	35.16	34.56	11	13887	670	56277499
Disseminated tuberculosis	35.06	34.56	16	13882	2767	56275402
Cellulitis staphylococcal	34.80	34.56	11	13887	693	56277476
Escherichia bacteraemia	34.71	34.56	17	13881	3443	56274726
Gastroenteritis adenovirus	34.63	34.56	8	13890	150	56278019

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
Acute graft versus host disease	957.73	24.65	281	17702	5872	31673489
Graft versus host disease	885.63	24.65	300	17683	10147	31669214
Venoocclusive liver disease	843.28	24.65	266	17717	7146	31672215
Cytomegalovirus infection	799.84	24.65	352	17631	24355	31655006
Acute graft versus host disease in skin	631.82	24.65	193	17790	4639	31674722
Product use in unapproved indication	573.77	24.65	463	17520	98708	31580653
Venoocclusive disease	564.42	24.65	155	17828	2517	31676844
Mucosal inflammation	560.57	24.65	307	17676	34120	31645241
Chronic graft versus host disease	534.27	24.65	166	17817	4226	31675135
Cystitis haemorrhagic	452.17	24.65	153	17830	5136	31674225
Graft versus host disease in skin	319.02	24.65	107	17876	3490	31675871
Graft versus host disease in gastrointestinal tract	318.53	24.65	106	17877	3373	31675988
Epstein-Barr virus infection	277.13	24.65	115	17868	6838	31672523
Acute graft versus host disease in intestine	255.52	24.65	83	17900	2443	31676918
BK virus infection	250.45	24.65	98	17885	4997	31674364
Thrombotic microangiopathy	244.41	24.65	115	17868	9236	31670125
Cytomegalovirus viraemia	240.55	24.65	103	17880	6622	31672739
Posterior reversible encephalopathy syndrome	238.08	24.65	113	17870	9254	31670107
Post transplant lymphoproliferative disorder	237.10	24.65	99	17884	5977	31673384
Acute myeloid leukaemia recurrent	204.28	24.65	66	17917	1908	31677453
Transplant failure	200.29	24.65	73	17910	3053	31676308
Viral haemorrhagic cystitis	168.63	24.65	49	17934	982	31678379
Febrile neutropenia	164.02	24.65	267	17716	121582	31557779
Multiple organ dysfunction syndrome	146.91	24.65	187	17796	68016	31611345
End stage renal disease	141.89	24.65	76	17907	8033	31671328
Cytomegalovirus infection reactivation	136.60	24.65	59	17924	3870	31675491
Adenovirus infection	135.16	24.65	62	17921	4692	31674669
Herpes simplex	129.35	24.65	62	17921	5183	31674178
Bacteraemia	120.10	24.65	91	17892	17543	31661818
Fatigue	115.21	24.65	25	17958	335181	31344180
Stomatitis	112.72	24.65	125	17858	39313	31640048
Bronchopulmonary aspergillosis	107.82	24.65	77	17906	13557	31665804
Acute graft versus host disease in liver	105.75	24.65	37	17946	1371	31677990
Off label use	104.95	24.65	431	17552	346843	31332518
JC virus infection	103.80	24.65	40	17943	1954	31677407
Progressive multifocal leukoencephalopathy	99.15	24.65	63	17920	9150	31670211
Leukaemia recurrent	97.39	24.65	36	17947	1566	31677795
Chronic graft versus host disease in skin	93.00	24.65	30	17953	862	31678499
Bone marrow transplant rejection	88.55	24.65	21	17962	181	31679180
Pneumonia cytomegaloviral	86.87	24.65	39	17944	2805	31676556
Cystitis viral	85.93	24.65	25	17958	503	31678858
Cytomegalovirus test positive	84.01	24.65	41	17942	3564	31675797
Aplastic anaemia	82.16	24.65	56	17927	9147	31670214
Respiratory failure	82.07	24.65	179	17804	101270	31578091
Engraftment syndrome	80.40	24.65	27	17956	882	31678479
Dizziness	79.03	24.65	10	17973	199137	31480224
Acute lymphocytic leukaemia recurrent	76.72	24.65	37	17946	3133	31676228
Human herpesvirus 6 infection	76.69	24.65	32	17951	1925	31677436
Blood follicle stimulating hormone increased	76.44	24.65	18	17965	150	31679211
Engraft failure	76.26	24.65	22	17961	429	31678932
Pancytopenia	73.96	24.65	157	17826	87159	31592202
Acute myeloid leukaemia	72.87	24.65	70	17913	18602	31660759
Fall	72.26	24.65	10	17973	186079	31493282
Stenotrophomonas infection	70.89	24.65	30	17953	1870	31677491
Asthenia	67.17	24.65	22	17961	224733	31454628
Chronic graft versus host disease in liver	66.98	24.65	19	17964	348	31679013
Graft versus host disease in liver	66.40	24.65	25	17958	1145	31678216
Bone marrow failure	63.70	24.65	79	17904	27929	31651432
Epstein-Barr virus infection reactivation	62.85	24.65	22	17961	816	31678545
Stem cell transplant	62.28	24.65	28	17955	2020	31677341
Arthralgia	61.53	24.65	7	17976	151417	31527944
Dyspnoea	61.22	24.65	63	17920	343416	31335945
Blood luteinising hormone increased	57.97	24.65	13	17970	85	31679276
Autoimmune lymphoproliferative syndrome	56.12	24.65	14	17969	152	31679209
Epstein-Barr virus associated lymphoproliferative disorder	55.91	24.65	25	17958	1781	31677580
Idiopathic pneumonia syndrome	55.31	24.65	15	17968	231	31679130
Obliterative bronchiolitis	55.12	24.65	22	17961	1180	31678181
Autoimmune haemolytic anaemia	53.72	24.65	32	17951	4140	31675221
Human herpesvirus 6 encephalitis	50.49	24.65	14	17969	235	31679126
Product dose omission issue	48.01	24.65	3	17980	105583	31573778
Epstein-Barr viraemia	47.52	24.65	19	17964	1024	31678337
Death	47.11	24.65	83	17900	360486	31318875
Polyomavirus viraemia	46.30	24.65	17	17966	725	31678636
Encephalitis	46.00	24.65	35	17948	6780	31672581
Meningitis tuberculous	44.13	24.65	16	17967	658	31678703
Toxoplasmosis	43.52	24.65	19	17964	1278	31678083
Cerebral toxoplasmosis	43.05	24.65	20	17963	1557	31677804
Mucormycosis	42.97	24.65	31	17952	5539	31673822
Constipation	42.94	24.65	9	17974	123982	31555379
Complications of bone marrow transplant	42.39	24.65	12	17971	218	31679143
Chronic graft versus host disease in intestine	41.45	24.65	12	17971	237	31679124
Bone marrow transplant	41.41	24.65	17	17966	981	31678380
Pulmonary haemorrhage	41.25	24.65	38	17945	9577	31669784
Poikiloderma	41.14	24.65	11	17972	160	31679201
Acute respiratory distress syndrome	40.18	24.65	59	17924	24481	31654880
Infection reactivation	39.63	24.65	18	17965	1330	31678031
Tooth development disorder	37.99	24.65	7	17976	13	31679348
Blood bilirubin increased	37.93	24.65	70	17913	35066	31644295
Weight decreased	37.70	24.65	22	17961	159930	31519431
Diffuse alveolar damage	37.44	24.65	20	17963	2099	31677262
Gastrointestinal mucosal disorder	36.83	24.65	12	17971	356	31679005
Chloroma	36.08	24.65	13	17970	525	31678836
Transplant rejection	35.25	24.65	35	17948	9673	31669688
Anxiety	35.03	24.65	5	17978	91028	31588333
Haemophagocytic lymphohistiocytosis	35.03	24.65	38	17945	11640	31667721
Ascites	34.96	24.65	74	17909	40939	31638422
Chronic myeloid leukaemia recurrent	34.95	24.65	10	17973	189	31679172
Pain	34.61	24.65	33	17950	186726	31492635
Cardiotoxicity	34.33	24.65	26	17957	5001	31674360
Overdose	34.14	24.65	4	17979	84660	31594701
Hepatic vein occlusion	34.11	24.65	9	17974	124	31679237
Myocardial infarction	34.01	24.65	11	17972	113443	31565918
Chest pain	33.92	24.65	12	17971	116945	31562416
Hepatic failure	33.86	24.65	64	17919	32638	31646723
Pain in extremity	33.56	24.65	12	17971	116191	31563170
Pulmonary alveolar haemorrhage	33.50	24.65	29	17954	6737	31672624
Enterococcal bacteraemia	32.87	24.65	17	17966	1671	31677690
Eccrine squamous syringometaplasia	32.81	24.65	7	17976	35	31679326
Pruritus	32.78	24.65	15	17968	125152	31554209
Septic shock	32.73	24.65	97	17886	66061	31613300
Insomnia	32.59	24.65	7	17976	94829	31584532
Retinopathy haemorrhagic	32.02	24.65	7	17976	40	31679321
Reticulocytosis	31.83	24.65	10	17973	263	31679098
Evans syndrome	31.80	24.65	10	17973	264	31679097
Dysbiosis	31.79	24.65	11	17972	394	31678967
Blood pressure increased	31.53	24.65	4	17979	79629	31599732
Pneumocystis jirovecii pneumonia	31.50	24.65	45	17938	18206	31661155
Pathogen resistance	30.91	24.65	31	17952	8670	31670691
Depression	30.61	24.65	7	17976	90808	31588553
Pyrexia	30.53	24.65	284	17699	303556	31375805
Sepsis	30.50	24.65	168	17815	151761	31527600
Stenotrophomonas bacteraemia	30.32	24.65	7	17976	53	31679308
Myalgia	30.30	24.65	4	17979	77254	31602107
Cytopenia	29.88	24.65	34	17949	10976	31668385
Hyperfibrinogenaemia	29.87	24.65	7	17976	57	31679304
Back pain	28.82	24.65	13	17970	109400	31569961
Haptoglobin decreased	28.70	24.65	11	17972	529	31678832
Second primary malignancy	28.63	24.65	27	17956	7005	31672356
Dehydration	28.60	24.65	16	17967	119095	31560266
Rash	28.44	24.65	44	17939	201442	31477919
Primary hypogonadism	28.40	24.65	7	17976	72	31679289
Neurological decompensation	28.34	24.65	18	17965	2609	31676752
Graft versus host disease in eye	28.32	24.65	9	17974	246	31679115
Myelodysplastic syndrome	28.26	24.65	44	17939	19207	31660154
Neurotoxicity	28.00	24.65	40	17943	16186	31663175
Adenomatous polyposis coli	27.97	24.65	8	17975	151	31679210
Malaise	27.61	24.65	33	17950	168478	31510883
Pseudomonal sepsis	27.46	24.65	19	17964	3177	31676184
Disseminated toxoplasmosis	27.34	24.65	6	17977	35	31679326
Skin toxicity	27.28	24.65	21	17962	4138	31675223
Acanthamoeba infection	27.07	24.65	10	17973	434	31678927
Coombs direct test positive	26.74	24.65	9	17974	296	31679065
Haematotoxicity	26.41	24.65	26	17957	7111	31672250
Hypodontia	25.90	24.65	4	17979	0	31679361
Encephalitis cytomegalovirus	25.49	24.65	10	17973	512	31678849
Drug interaction	25.38	24.65	50	17933	208493	31470868
Staphylococcal bacteraemia	25.19	24.65	26	17957	7522	31671839
Angiodysplasia	25.01	24.65	10	17973	539	31678822
Thrombocytopenia	24.83	24.65	152	17831	142595	31536766
Blood bilirubin unconjugated increased	24.73	24.65	10	17973	555	31678806
Anti-platelet antibody positive	24.66	24.65	8	17975	234	31679127

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
Acute graft versus host disease	1830.75	25.43	485	30380	9077	70888502
Graft versus host disease	1696.47	25.43	504	30361	14519	70883060
Venoocclusive liver disease	1638.74	25.43	455	30410	10223	70887356
Cytomegalovirus infection	1600.62	25.43	614	30251	39144	70858435
Chronic graft versus host disease	1265.02	25.43	337	30528	6433	70891146
Product use in unapproved indication	1142.08	25.43	844	30021	206634	70690945
Acute graft versus host disease in skin	1135.52	25.43	313	30552	6824	70890755
Mucosal inflammation	1034.05	25.43	530	30335	67320	70830259
Venoocclusive disease	879.89	25.43	229	30636	3971	70893608
Cystitis haemorrhagic	775.99	25.43	243	30622	8350	70889229
Graft versus host disease in skin	701.21	25.43	204	30661	5426	70892153
Graft versus host disease in gastrointestinal tract	599.54	25.43	183	30682	5761	70891818
Cytomegalovirus viraemia	540.11	25.43	200	30665	11485	70886094
Acute graft versus host disease in intestine	491.69	25.43	142	30723	3674	70893905
Post transplant lymphoproliferative disorder	467.27	25.43	175	30690	10370	70887209
Thrombotic microangiopathy	448.32	25.43	197	30668	17651	70879928
Epstein-Barr virus infection	439.44	25.43	178	30687	13020	70884559
BK virus infection	396.02	25.43	144	30721	7845	70889734
Acute myeloid leukaemia recurrent	395.04	25.43	114	30751	2940	70894639
Posterior reversible encephalopathy syndrome	340.55	25.43	180	30685	24222	70873357
Febrile neutropenia	332.22	25.43	426	30439	203892	70693687
Viral haemorrhagic cystitis	331.63	25.43	89	30776	1742	70895837
Cytomegalovirus infection reactivation	316.73	25.43	117	30748	6664	70890915
Adenovirus infection	301.26	25.43	117	30748	7651	70889928
Transplant failure	292.36	25.43	97	30768	4010	70893569
Multiple organ dysfunction syndrome	250.55	25.43	271	30594	108244	70789335
Bacteraemia	247.71	25.43	156	30709	29153	70868426
Acute graft versus host disease in liver	236.69	25.43	68	30797	1724	70895855
Chronic graft versus host disease in skin	226.83	25.43	63	30802	1408	70896171
Ovarian failure	225.53	25.43	52	30813	526	70897053
Herpes simplex	215.99	25.43	103	30762	11129	70886450
Off label use	208.21	25.43	751	30114	742309	70155270
Leukaemia recurrent	191.37	25.43	64	30801	2711	70894868
Acute lymphocytic leukaemia recurrent	190.63	25.43	74	30791	4830	70892749
Cystitis viral	186.46	25.43	46	30819	634	70896945
Premature menopause	185.29	25.43	44	30821	511	70897068
Blood follicle stimulating hormone increased	180.33	25.43	39	30826	286	70897293
Fatigue	175.69	25.43	70	30795	824249	70073330
Blood luteinising hormone increased	167.20	25.43	34	30831	177	70897402
Human herpesvirus 6 infection	166.73	25.43	67	30798	4792	70892787
Aplastic anaemia	164.27	25.43	98	30767	16618	70880961
Pancytopenia	163.80	25.43	260	30605	150847	70746732
Ovarian atrophy	162.03	25.43	29	30836	63	70897516
Idiopathic pneumonia syndrome	158.87	25.43	39	30826	526	70897053
Acute myeloid leukaemia	151.78	25.43	118	30747	30822	70866757
Dizziness	148.54	25.43	15	30850	464126	70433453
Arthralgia	147.12	25.43	22	30843	503368	70394211
JC virus infection	139.50	25.43	54	30811	3497	70894082
End stage renal disease	138.15	25.43	76	30789	11057	70886522
Fall	135.43	25.43	17	30848	444079	70453500
Bone marrow transplant rejection	130.78	25.43	29	30836	242	70897337
Cytomegalovirus test positive	129.25	25.43	58	30807	5450	70892129
Stem cell transplant	128.44	25.43	51	30814	3534	70894045
Bronchopulmonary aspergillosis	127.39	25.43	91	30774	20911	70876668
Toxoplasmosis	125.43	25.43	46	30819	2564	70895015
Pulmonary haemorrhage	123.63	25.43	76	30789	13597	70883982
Progressive multifocal leukoencephalopathy	120.58	25.43	85	30780	19129	70878450
Stomatitis	117.59	25.43	205	30660	128306	70769273
Pain	117.36	25.43	64	30801	628752	70268827
Respiratory failure	116.94	25.43	239	30626	168496	70729083
Pneumonia cytomegaloviral	110.13	25.43	49	30816	4512	70893067
Primary hypogonadism	108.17	25.43	23	30842	154	70897425
Epstein-Barr viraemia	107.86	25.43	38	30827	1885	70895694
Bone marrow failure	105.34	25.43	118	30747	48892	70848687
Engraft failure	104.96	25.43	29	30836	635	70896944
Pain in extremity	103.85	25.43	11	30854	328071	70569508
Thrombocytopenia	103.73	25.43	282	30583	238828	70658751
Mucormycosis	100.23	25.43	55	30810	7959	70889620
Chronic graft versus host disease in liver	98.43	25.43	27	30838	575	70897004
Neurotoxicity	95.43	25.43	89	30776	29737	70867842
Asthenia	92.19	25.43	42	30823	457624	70439955
Drug hypersensitivity	90.72	25.43	6	30859	262453	70635126
Engraftment syndrome	90.53	25.43	30	30835	1234	70896345
Peripheral swelling	89.50	25.43	3	30862	236560	70661019
Dyspnoea	88.55	25.43	124	30741	769936	70127643
Graft versus host disease in liver	87.05	25.43	31	30834	1587	70895992
Headache	87.02	25.43	75	30790	580330	70317249
Bacterial sepsis	86.15	25.43	49	30816	7598	70889981
Haemophagocytic lymphohistiocytosis	83.81	25.43	69	30796	19543	70878036
Encephalitis cytomegalovirus	83.45	25.43	27	30838	1029	70896550
Acute respiratory distress syndrome	83.01	25.43	96	30769	41158	70856421
Graft versus host disease in lung	81.60	25.43	25	30840	795	70896784
Product dose omission issue	81.42	25.43	3	30862	217465	70680114
Transplant dysfunction	79.80	25.43	45	30820	6864	70890715
Complications of bone marrow transplant	78.95	25.43	23	30842	613	70896966
Epstein-Barr virus associated lymphoproliferative disorder	78.34	25.43	35	30830	3254	70894325
Pruritus	77.25	25.43	27	30838	345533	70552046
Nasopharyngitis	77.02	25.43	5	30860	222201	70675378
Abdominal discomfort	76.94	25.43	4	30861	214654	70682925
Adenoviral hepatitis	76.66	25.43	24	30841	821	70896758
Cerebral toxoplasmosis	75.95	25.43	30	30835	2050	70895529
Stenotrophomonas infection	74.57	25.43	34	30831	3315	70894264
Upper respiratory fungal infection	74.43	25.43	19	30846	303	70897276
Systemic mycosis	73.68	25.43	31	30834	2491	70895088
Obliterative bronchiolitis	73.20	25.43	32	30833	2825	70894754
Autoimmune haemolytic anaemia	72.44	25.43	44	30821	7702	70889877
Human polyomavirus infection	71.63	25.43	24	30841	1022	70896557
Cytomegalovirus chorioretinitis	70.81	25.43	38	30827	5260	70892319
Epstein-Barr virus infection reactivation	70.20	25.43	26	30839	1490	70896089
Back pain	70.19	25.43	16	30849	271136	70626443
Pulmonary veno-occlusive disease	69.86	25.43	26	30839	1510	70896069
Infusion related reaction	69.80	25.43	4	30861	197530	70700049
Transplant rejection	69.55	25.43	60	30805	18111	70879468
Anxiety	68.13	25.43	8	30857	220322	70677257
Sepsis	67.72	25.43	247	30618	244298	70653281
Pyrexia	67.45	25.43	473	30392	606479	70291100
Human herpesvirus 6 encephalitis	66.18	25.43	19	30846	480	70897099
Ascites	64.67	25.43	110	30755	67437	70830142
Chronic graft versus host disease in intestine	64.15	25.43	17	30848	316	70897263
Septic shock	63.95	25.43	147	30718	112111	70785468
Disseminated toxoplasmosis	63.74	25.43	15	30850	167	70897412
Neoplasm recurrence	63.37	25.43	32	30833	3909	70893670
Myelodysplastic syndrome	62.77	25.43	71	30794	29714	70867865
Bone marrow transplant	62.05	25.43	23	30842	1321	70896258
Drug resistance	60.84	25.43	79	30786	38111	70859468
Blood stem cell transplant failure	60.50	25.43	18	30847	517	70897062
Swelling	60.45	25.43	6	30859	188533	70709046
Polyomavirus viraemia	59.26	25.43	22	30843	1269	70896310
Hepatic vein occlusion	59.16	25.43	14	30851	160	70897419
Malaise	58.87	25.43	61	30804	432871	70464708
Pulmonary alveolar haemorrhage	58.48	25.43	43	30822	10326	70887253
Aspergillus infection	58.46	25.43	54	30811	17814	70879765
Autoimmune lymphoproliferative syndrome	58.01	25.43	14	30851	175	70897404
Constipation	57.65	25.43	19	30846	252419	70645160
Rash	56.78	25.43	84	30781	510478	70387101
Hepatic failure	56.69	25.43	95	30770	57530	70840049
Hypersensitivity	56.66	25.43	15	30850	229797	70667782
Syncope	56.62	25.43	4	30861	165705	70731874
Weight decreased	55.76	25.43	33	30832	310455	70587124
Infection reactivation	55.71	25.43	25	30840	2348	70895231
Nausea	55.65	25.43	188	30677	851900	70045679
Urticaria	55.52	25.43	4	30861	163045	70734534
Chest pain	55.49	25.43	20	30845	251240	70646339
Recurrent cancer	55.03	25.43	25	30840	2416	70895163
Myalgia	54.73	25.43	5	30860	167887	70729692
Encephalitis	54.32	25.43	46	30819	13539	70884040
Seizure	53.73	25.43	185	30680	177777	70719802
Myelitis	53.49	25.43	24	30841	2253	70895326
Blood pressure increased	53.23	25.43	9	30856	188508	70709071
Pseudomonal sepsis	53.19	25.43	32	30833	5505	70892074
Staphylococcal sepsis	52.73	25.43	45	30820	13382	70884197
Respiratory distress	52.31	25.43	89	30776	54561	70843018
Insomnia	52.23	25.43	15	30850	217791	70679788
Gait disturbance	51.91	25.43	9	30856	185097	70712482
Cardiotoxicity	51.64	25.43	41	30824	11029	70886550
Laryngitis fungal	51.46	25.43	12	30853	128	70897451
Somnolence	51.42	25.43	15	30850	215591	70681988
Depression	50.96	25.43	12	30853	198962	70698617
Hepatomegaly	49.88	25.43	49	30816	17443	70880136
Alternaria infection	49.67	25.43	16	30849	601	70896978
Candida sepsis	49.59	25.43	23	30842	2332	70895247
Enterococcal bacteraemia	49.37	25.43	24	30841	2702	70894877
Pathogen resistance	49.11	25.43	43	30822	13236	70884343
Staphylococcal infection	48.53	25.43	85	30780	53319	70844260
Graft versus host disease in eye	46.44	25.43	13	30852	299	70897280
Tooth hypoplasia	46.23	25.43	12	30853	205	70897374
Chloroma	46.22	25.43	16	30849	753	70896826
Pneumocystis jirovecii pneumonia	46.01	25.43	61	30804	30021	70867558
Mucosal disorder	45.74	25.43	24	30841	3174	70894405
Cytopenia	44.76	25.43	46	30819	17277	70880302
Myocardial infarction	44.65	25.43	10	30855	171635	70725944
Hypotension	44.47	25.43	67	30798	404314	70493265
Condition aggravated	44.05	25.43	74	30791	427561	70470018
Overdose	43.94	25.43	10	30855	169735	70727844
Neutropenia	43.57	25.43	224	30641	256932	70640647
Dehydration	43.54	25.43	22	30843	226120	70671459
Gastroenteritis adenovirus	43.50	25.43	12	30853	261	70897318
Growth retardation	43.50	25.43	19	30846	1673	70895906
Abdominal pain upper	43.44	25.43	15	30850	193587	70703992
Hyperhidrosis	42.66	25.43	4	30861	131582	70765997
Meningoencephalitis herpetic	41.98	25.43	19	30846	1820	70895759
Diffuse alveolar damage	41.83	25.43	23	30842	3340	70894239
Synovitis	41.71	25.43	4	30861	129224	70768355
Systemic candida	41.33	25.43	28	30837	5906	70891673
Disseminated mucormycosis	40.85	25.43	14	30851	639	70896940
Product administration error	40.81	25.43	57	30808	29466	70868113
Blood bilirubin increased	40.42	25.43	84	30781	59817	70837762
Haematotoxicity	40.29	25.43	39	30826	13635	70883944
Hepatic necrosis	40.28	25.43	32	30833	8614	70888965
Clostridium difficile colitis	40.10	25.43	56	30809	28940	70868639
Poikiloderma	40.06	25.43	12	30853	353	70897226
Urinary tract infection	39.86	25.43	30	30835	248739	70648840
Meningitis tuberculous	39.32	25.43	16	30849	1181	70896398
Renal failure	38.74	25.43	174	30691	188896	70708683
Fungal infection	38.50	25.43	63	30802	37404	70860175
Cerebrovascular accident	38.04	25.43	8	30857	143462	70754117
Fungaemia	37.69	25.43	23	30842	4059	70893520
Staphylococcal bacteraemia	37.24	25.43	34	30831	11048	70886531
Myelosuppression	36.98	25.43	55	30810	30090	70867489
Respiratory tract infection fungal	36.47	25.43	15	30850	1138	70896441
Drug intolerance	36.43	25.43	27	30838	225660	70671919
Aplasia	36.29	25.43	28	30837	7223	70890356
Pneumonia respiratory syncytial viral	36.04	25.43	16	30849	1465	70896114
Sweat gland tumour	35.92	25.43	12	30853	506	70897073
Asthma	35.84	25.43	5	30860	120788	70776791
Eccrine squamous syringometaplasia	35.35	25.43	7	30858	31	70897548
Sinusitis	34.82	25.43	15	30850	169180	70728399
Pericardial effusion	34.76	25.43	64	30801	41712	70855867
Pneumonia fungal	34.36	25.43	31	30834	9922	70887657
Alopecia	34.35	25.43	22	30843	198468	70699111
Neutropenic infection	34.33	25.43	17	30848	1992	70895587
Aplasia pure red cell	33.73	25.43	27	30838	7347	70890232
Citrobacter bacteraemia	33.53	25.43	6	30859	13	70897566
Confusional state	33.33	25.43	45	30820	284353	70613226
Tooth development disorder	32.90	25.43	7	30858	47	70897532
Enterococcal infection	32.85	25.43	36	30829	14546	70883033
Immune thrombocytopenia	32.85	25.43	38	30827	16286	70881293
General physical health deterioration	32.32	25.43	33	30832	235998	70661581
Reticulocytosis	32.29	25.43	11	30854	493	70897086
Haptoglobin decreased	31.32	25.43	14	30851	1303	70896276
Disseminated intravascular coagulation	31.20	25.43	54	30811	33544	70864035
Coombs direct test positive	30.76	25.43	10	30855	387	70897192
Retinopathy haemorrhagic	30.61	25.43	7	30858	68	70897511
Refractoriness to platelet transfusion	30.54	25.43	8	30857	142	70897437
Device related infection	30.24	25.43	52	30813	32133	70865446
Hypoglycaemia	30.24	25.43	3	30862	94361	70803218
Cardiac tamponade	30.12	25.43	27	30838	8568	70889011
Skin toxicity	30.07	25.43	25	30840	7173	70890406
Oedema peripheral	29.99	25.43	33	30832	228058	70669521
Lymphoproliferative disorder	29.82	25.43	22	30843	5307	70892272
Pseudomonas infection	29.79	25.43	39	30826	18955	70878624
Anti-platelet antibody positive	29.75	25.43	9	30856	274	70897305
Memory impairment	29.54	25.43	3	30862	92638	70804941
Tooth malformation	29.50	25.43	7	30858	81	70897498
Metapneumovirus infection	29.40	25.43	14	30851	1506	70896073
Disease recurrence	29.29	25.43	56	30809	37547	70860032
Nodular melanoma	29.22	25.43	8	30857	169	70897410
Blood bilirubin unconjugated increased	29.14	25.43	12	30853	913	70896666
Hyperfibrinogenaemia	29.11	25.43	7	30858	86	70897493
Bradycardia	29.10	25.43	9	30856	124606	70772973
Focal nodular hyperplasia	28.93	25.43	11	30854	678	70896901
Dysbiosis	28.91	25.43	12	30853	932	70896647
Gastrooesophageal reflux disease	28.82	25.43	3	30862	90836	70806743
Pulmonary hypertension	28.78	25.43	63	30802	46473	70851106
Encephalitis viral	28.46	25.43	16	30849	2426	70895153
Primary adrenal insufficiency	28.38	25.43	8	30857	189	70897390
Organising pneumonia	28.37	25.43	28	30837	10022	70887557
Iron overload	28.28	25.43	14	30851	1639	70895940
Adenomatous polyposis coli	28.18	25.43	8	30857	194	70897385
Adenoviral haemorrhagic cystitis	28.08	25.43	10	30855	512	70897067
Acanthamoeba infection	27.76	25.43	10	30855	529	70897050
Palpitations	27.72	25.43	7	30858	110746	70786833
BK polyomavirus test positive	27.58	25.43	7	30858	109	70897470
Hyponatraemia	27.35	25.43	18	30847	160069	70737510
Second primary malignancy	27.30	25.43	31	30834	13020	70884559
Haemolysis	26.86	25.43	29	30836	11522	70886057
Adrenal haemorrhage	26.80	25.43	10	30855	585	70896994
Muscle spasms	26.75	25.43	17	30848	154029	70743550
Hypoaesthesia	26.65	25.43	17	30848	153722	70743857
Colitis herpes	26.53	25.43	5	30860	16	70897563
Bacterial infection	26.48	25.43	44	30821	26448	70871131
Candida infection	26.43	25.43	51	30814	34422	70863157
Delayed engraftment	26.31	25.43	8	30857	248	70897331
Gastrointestinal toxicity	26.25	25.43	22	30843	6383	70891196
Leukoencephalopathy	25.73	25.43	23	30842	7271	70890308
Hilar lymphadenopathy	25.73	25.43	13	30852	1590	70895989
Herpes simplex viraemia	25.57	25.43	8	30857	273	70897306

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01AB01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS ALKYLATING AGENTS Alkyl sulfonates
FDA MoA	N0000000236	Alkylating Activity
FDA EPC	N0000175558	Alkylating Drug
MeSH PA	D000477	Alkylating Agents
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D018906	Antineoplastic Agents, Alkylating
MeSH PA	D007155	Immunologic Factors
MeSH PA	D007166	Immunosuppressive Agents
MeSH PA	D019653	Myeloablative Agonists
MeSH PA	D009676	Noxae
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:50903	carcinogen
CHEBI has role	CHEBI:50905	teratogeno
CHEBI has role	CHEBI:67105	insect sterilants

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

Disease	Relation	SNOMED_ID	DOID
Allogeneic bone marrow transplantation	indication	58390007
Malignant lymphoma	indication	118600007	DOID:0060058
Neuroblastoma	indication	432328008	DOID:769
Autologous hematopoietic stem-cell transplantation for Ewing's sarcoma family of tumors	indication	709115004
Philadelphia Chromosome Positive Chronic Myelocytic Leukemia	indication
Mycosis	contraindication	3218000	DOID:1564
Fanconi's anemia	contraindication	30575002	DOID:13636
Viral disease	contraindication	34014006	DOID:934
Hyperuricemia	contraindication	35885006	DOID:1920
Hypokalemia	contraindication	43339004
Fibrosis of lung	contraindication	51615001	DOID:3770
Portal vein obstruction	contraindication	57348003
Hyperglycemia	contraindication	80394007	DOID:4195
Epilepsy	contraindication	84757009	DOID:1826
Bacterial infectious disease	contraindication	87628006
Radiation oncology AND/OR radiotherapy	contraindication	108290001
Hypomagnesemia	contraindication	190855004
Anemia	contraindication	271737000	DOID:2355
Pregnancy, function	contraindication	289908002
Thrombocytopenic disorder	contraindication	302215000	DOID:1588
Neutropenic disorder	contraindication	303011007	DOID:1227
Breastfeeding (mother)	contraindication	413712001
Severe Bone Marrow Depression	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Matrix metalloproteinase-9	Enzyme	P14780	MMP9_HUMAN		IC50	5.28		DRUG MATRIX

External reference:

ID	Source
4018773	VUID
N0000147076	NUI
D00248	KEGG_DRUG
1828	RXNORM
4018773	VANDF
C0006463	UMLSCUI
CHEBI:28901	CHEBI
CHEMBL820	ChEMBL_ID
DB01008	DRUGBANK_ID
D002066	MESH_DESCRIPTOR_UI
2478	PUBCHEM_CID
7136	IUPHAR_LIGAND_ID
564	INN_ID
G1LN9045DK	UNII
121305	MMSL
37850	MMSL
4309	MMSL
d00183	MMSL
002638	NDDF
2571007	SNOMEDCT_US
387138002	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
BUSULFAN	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1112	INJECTION, SOLUTION	6 mg	INTRAVENOUS	ANDA	28 sections
BUSULFAN	HUMAN PRESCRIPTION DRUG LABEL	1	0517-0920	INJECTION	6 mg	INTRAVENOUS	ANDA	27 sections
Busulfan	HUMAN PRESCRIPTION DRUG LABEL	1	16729-351	INJECTION	6 mg	INTRAVENOUS	ANDA	27 sections
Busulfan	HUMAN PRESCRIPTION DRUG LABEL	1	25021-241	INJECTION, SOLUTION, CONCENTRATE	6 mg	INTRAVENOUS	ANDA	27 sections
Busulfan	HUMAN PRESCRIPTION DRUG LABEL	1	25021-241	INJECTION, SOLUTION, CONCENTRATE	6 mg	INTRAVENOUS	ANDA	27 sections
Busulfan	HUMAN PRESCRIPTION DRUG LABEL	1	51817-170	INJECTION	6 mg	INTRAVENOUS	ANDA	28 sections
Busulfan	HUMAN PRESCRIPTION DRUG LABEL	1	51817-170	INJECTION	6 mg	INTRAVENOUS	ANDA	28 sections
BUSULFEX	HUMAN PRESCRIPTION DRUG LABEL	1	59148-070	INJECTION	6 mg	INTRAVENOUS	NDA	28 sections
Busulfan	HUMAN PRESCRIPTION DRUG LABEL	1	60505-6177	INJECTION	6 mg	INTRAVENOUS	ANDA	27 sections
Busulfan	HUMAN PRESCRIPTION DRUG LABEL	1	65219-160	INJECTION	6 mg	INTRAVENOUS	ANDA	27 sections
Busulfan	HUMAN PRESCRIPTION DRUG LABEL	1	67457-893	INJECTION	6 mg	INTRAVENOUS	ANDA	28 sections
MYLERAN	HUMAN PRESCRIPTION DRUG LABEL	1	69784-620	TABLET, FILM COATED	2 mg	ORAL	NDA	23 sections
Busulfan	HUMAN PRESCRIPTION DRUG LABEL	1	70121-1244	INJECTION	6 mg	INTRAVENOUS	ANDA	27 sections
Busulfan	HUMAN PRESCRIPTION DRUG LABEL	1	71288-116	INJECTION, SOLUTION	6 mg	INTRAVENOUS	ANDA	27 sections
Busulfan	HUMAN PRESCRIPTION DRUG LABEL	1	71288-158	INJECTION, SOLUTION	6 mg	INTRAVENOUS	ANDA	28 sections
Busulfan	HUMAN PRESCRIPTION DRUG LABEL	1	72485-210	INJECTION, SOLUTION	6 mg	INTRAVENOUS	ANDA	28 sections
Busulfan	HUMAN PRESCRIPTION DRUG LABEL	1	72606-559	INJECTION	6 mg	INTRAVENOUS	ANDA	28 sections
MYLERAN	HUMAN PRESCRIPTION DRUG LABEL	1	76388-713	TABLET, FILM COATED	2 mg	ORAL	NDA	23 sections
MYLERAN	HUMAN PRESCRIPTION DRUG LABEL	1	76388-713	TABLET, FILM COATED	2 mg	ORAL	NDA	23 sections