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

Stem definition	Drug id	CAS RN
	1399	127-07-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: xromi siklos hydroxyurea biosupressin carbamohydroxamic acid carbamohydroximic acid carbamoyl oxime oxyrea oxyurea hydroxycarbamide	An antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. Molecular weight: 76.06 Formula: CH4N2O2 CLOGP: -1.80 LIPINSKI: 0 HAC: 4 HDO: 3 TPSA: 75.35 ALOGS: 0.55 ROTB: 0

Molecule

Description

Molfile Inchi Smiles

Synonyms:

xromi
siklos
hydroxyurea
biosupressin
carbamohydroxamic acid
carbamohydroximic acid
carbamoyl oxime
oxyrea
oxyurea
hydroxycarbamide

An antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase.

Molecular weight: 76.06
Formula: CH4N2O2
CLOGP: -1.80
LIPINSKI: 0
HAC: 4
HDO: 3
TPSA: 75.35
ALOGS: 0.55
ROTB: 0

Drug dosage:

None

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	50 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	80 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1502.57 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	79 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.52 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	1.50 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
July 1, 2019	EMA	NOVA LABORATORIES IRELAND LIMITED
Dec. 7, 1967	FDA	BRISTOL MYERS SQUIBB

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
Sickle cell anaemia with crisis	437.11	14.42	123	14517	4420	50586064
Platelet count increased	218.21	14.42	99	14541	14441	50576043
Acute myeloid leukaemia	163.16	14.42	82	14558	14992	50575492
Splenomegaly	111.77	14.42	55	14585	9605	50580879
Acute chest syndrome	102.09	14.42	26	14614	631	50589853
Blast crisis in myelogenous leukaemia	98.27	14.42	24	14616	488	50589996
Myelofibrosis	96.55	14.42	28	14612	1119	50589365
Thrombocytopenia	96.19	14.42	149	14491	127524	50462960
White blood cell count increased	94.22	14.42	86	14554	42154	50548330
Pancytopenia	89.87	14.42	116	14524	83914	50506570
Thrombocytosis	87.72	14.42	38	14602	4958	50585526
Anaemia	83.35	14.42	208	14432	252248	50338236
Serum ferritin increased	83.03	14.42	37	14603	5165	50585319
Haemoglobin decreased	81.54	14.42	138	14502	127078	50463406
Leukocytosis	77.47	14.42	59	14581	22520	50567964
Chronic myeloid leukaemia	75.38	14.42	27	14613	2129	50588355
Platelet count decreased	73.65	14.42	116	14524	100610	50489874
Differentiation syndrome	62.11	14.42	19	14621	914	50589570
Erythromelalgia	51.42	14.42	11	14629	120	50590364
Intentional product use issue	48.64	14.42	83	14557	76835	50513649
Blood lactate dehydrogenase increased	47.89	14.42	42	14598	19520	50570964
Angiokeratoma	45.06	14.42	10	14630	131	50590353
Philadelphia chromosome positive	44.46	14.42	12	14628	367	50590117
Blood iron increased	43.60	14.42	16	14624	1352	50589132
Haematocrit increased	41.27	14.42	17	14623	1957	50588527
Tumour lysis syndrome	41.01	14.42	26	14614	7395	50583089
Haemoglobin increased	39.83	14.42	19	14621	3096	50587388
Skin ulcer	39.67	14.42	50	14590	35268	50555216
Laryngitis	38.39	14.42	29	14611	10927	50579557
Myeloproliferative neoplasm	37.56	14.42	11	14629	455	50590029
Nail pigmentation	37.04	14.42	9	14631	179	50590305
Febrile neutropenia	36.98	14.42	85	14555	97582	50492902
Transformation to acute myeloid leukaemia	36.80	14.42	9	14631	184	50590300
Sinusitis	32.96	14.42	5	14635	170553	50419931
Joint swelling	32.76	14.42	15	14625	245271	50345213
Aquagenic pruritus	32.67	14.42	6	14634	27	50590457
Drug hypersensitivity	32.53	14.42	16	14624	250994	50339490
Cytogenetic analysis abnormal	32.46	14.42	11	14629	735	50589749
Leukaemia	31.98	14.42	17	14623	3482	50587002
Drug resistance	31.69	14.42	33	14607	18956	50571528
Immunodeficiency	30.73	14.42	29	14611	14799	50575685
Chronic myeloid leukaemia transformation	30.66	14.42	7	14633	105	50590379
Toxicity to various agents	29.96	14.42	12	14628	212487	50377997
Arthropathy	29.68	14.42	5	14635	157901	50432583
Blood bilirubin increased	29.27	14.42	41	14599	31997	50558487
Essential thrombocythaemia	28.54	14.42	7	14633	145	50590339
Decreased appetite	26.72	14.42	122	14518	200801	50389683
Malignant neoplasm progression	26.56	14.42	60	14580	68064	50522420
Platelet count abnormal	26.48	14.42	14	14626	2835	50587649
Squamous cell carcinoma	26.05	14.42	20	14620	7719	50582765
Contraindicated product administered	25.31	14.42	6	14634	148952	50441532
Laryngeal inflammation	24.16	14.42	6	14634	131	50590353
Leukostasis syndrome	24.14	14.42	5	14635	46	50590438
Bone marrow failure	23.25	14.42	34	14606	27590	50562894
Glossodynia	23.23	14.42	3	14637	115566	50474918
Drug ineffective	23.11	14.42	141	14499	819192	49771292
Haematocrit decreased	22.43	14.42	38	14602	34938	50555546
Injection site pain	22.04	14.42	3	14637	111021	50479463
Adenocarcinoma metastatic	21.90	14.42	5	14635	75	50590409
Tyrosine kinase mutation	21.78	14.42	4	14636	18	50590466
Infusion related reaction	21.66	14.42	11	14629	169546	50420938
Viral infection	21.14	14.42	34	14606	29952	50560532
Post cardiac arrest syndrome	20.82	14.42	4	14636	24	50590460
Splenic rupture	20.66	14.42	9	14631	1189	50589295
Pleural effusion	20.63	14.42	61	14579	81393	50509091
Sickle cell anaemia	20.11	14.42	7	14633	507	50589977
Tonsillitis bacterial	19.68	14.42	5	14635	120	50590364
Ventricular hypokinesia	19.67	14.42	13	14627	3967	50586517
Myelodysplastic syndrome	19.55	14.42	23	14617	15109	50575375
Red blood cell count decreased	19.41	14.42	35	14605	33800	50556684
Polycythaemia vera	18.98	14.42	5	14635	139	50590345
Left ventricular dysfunction	18.87	14.42	19	14621	10487	50579997
Extramedullary haemopoiesis	18.27	14.42	4	14636	49	50590435
Posterior reversible encephalopathy syndrome	18.15	14.42	22	14618	14906	50575578
Serum ferritin decreased	18.00	14.42	9	14631	1623	50588861
Anxiety	17.96	14.42	15	14625	177591	50412893
Blast cell count increased	17.87	14.42	6	14634	390	50590094
Normal newborn	17.66	14.42	15	14625	6676	50583808
Uterine atony	17.56	14.42	5	14635	187	50590297
Hypersensitivity	17.42	14.42	22	14618	215139	50375345
Discomfort	17.20	14.42	5	14635	108375	50482109
Therapeutic product effect decreased	17.11	14.42	9	14631	136041	50454443
Gene mutation	17.01	14.42	8	14632	1263	50589221
Retinopathy sickle cell	17.00	14.42	4	14636	69	50590415
Dermatitis bullous	16.75	14.42	15	14625	7158	50583326
Hypoperfusion	16.66	14.42	8	14632	1322	50589162
Cytogenetic abnormality	16.63	14.42	6	14634	483	50590001
Maternal exposure before pregnancy	15.70	14.42	13	14627	5584	50584900
Transfusion	15.66	14.42	19	14621	12886	50577598
Palmar erythema	15.44	14.42	8	14632	1555	50588929
Mucosal inflammation	15.24	14.42	35	14605	40107	50550377
Gene mutation identification test positive	14.89	14.42	4	14636	120	50590364
Disease progression	14.85	14.42	61	14579	95805	50494679
Wound	14.85	14.42	6	14634	105788	50484696
Neutropenic colitis	14.70	14.42	9	14631	2408	50588076
Hepatic vein thrombosis	14.68	14.42	4	14636	127	50590357
Graft versus host disease	14.61	14.42	13	14627	6153	50584331

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
Sickle cell anaemia with crisis	338.02	14.33	100	14332	2508	29557587
Differentiation syndrome	145.59	14.33	43	14389	1070	29559025
Acute myeloid leukaemia	142.78	14.33	93	14339	16420	29543675
Myelofibrosis	125.87	14.33	41	14391	1421	29558674
Blast crisis in myelogenous leukaemia	116.59	14.33	31	14401	518	29559577
White blood cell count increased	114.96	14.33	115	14317	37401	29522694
Splenomegaly	112.85	14.33	74	14358	13205	29546890
Chronic myeloid leukaemia	105.97	14.33	39	14393	1955	29558140
Tumour lysis syndrome	98.05	14.33	69	14363	13815	29546280
Platelet count increased	89.04	14.33	54	14378	8409	29551686
Cytogenetic analysis abnormal	87.76	14.33	25	14407	545	29559550
Philadelphia chromosome positive	72.39	14.33	19	14413	301	29559794
Leukocytosis	63.22	14.33	64	14368	21078	29539017
Thrombocytopenia	61.43	14.33	174	14258	134649	29425446
Haemoglobin decreased	60.64	14.33	151	14281	108224	29451871
Blast cell count increased	58.57	14.33	21	14411	976	29559119
Hyperleukocytosis	58.51	14.33	24	14408	1611	29558484
Anaemia	57.99	14.33	222	14210	200729	29359366
Skin ulcer	54.45	14.33	56	14376	18784	29541311
Serum ferritin increased	52.04	14.33	33	14399	5555	29554540
Myeloproliferative neoplasm	51.18	14.33	16	14416	484	29559611
Endocarditis noninfective	51.17	14.33	12	14420	116	29559979
Drug resistance	49.95	14.33	57	14375	21483	29538612
Granulomatous rosacea	49.35	14.33	12	14420	137	29559958
Acute chest syndrome	44.61	14.33	13	14419	308	29559787
Idiopathic intracranial hypertension	44.47	14.33	15	14417	580	29559515
Blood lactate dehydrogenase increased	36.59	14.33	46	14386	19163	29540932
Loss of therapeutic response	35.76	14.33	11	14421	315	29559780
Full blood count abnormal	35.26	14.33	40	14392	14973	29545122
Actinic keratosis	34.36	14.33	22	14410	3764	29556331
Platelet count decreased	33.74	14.33	120	14312	104552	29455543
Chronic myelomonocytic leukaemia	33.64	14.33	12	14420	549	29559546
Intentional product use issue	33.57	14.33	68	14364	42430	29517665
Antineutrophil cytoplasmic antibody positive	32.64	14.33	12	14420	599	29559496
Posterior reversible encephalopathy syndrome	32.13	14.33	30	14402	8946	29551149
Graft versus host disease in skin	31.57	14.33	20	14412	3359	29556736
Splenic infarction	31.00	14.33	16	14416	1823	29558272
Pleural effusion	29.97	14.33	90	14342	71818	29488277
Toxicity to various agents	28.14	14.33	26	14406	173635	29386460
Parainfluenzae virus infection	27.98	14.33	16	14416	2233	29557862
Second primary malignancy	27.11	14.33	24	14408	6681	29553414
Spermatogenesis abnormal	26.07	14.33	6	14426	53	29560042
Subacute combined cord degeneration	25.05	14.33	7	14425	142	29559953
Pyrexia	23.24	14.33	228	14204	287394	29272701
Mucosal inflammation	23.12	14.33	49	14383	31546	29528549
Red blood cell count decreased	22.67	14.33	43	14389	25559	29534536
Erythropoiesis abnormal	22.45	14.33	7	14425	210	29559885
Completed suicide	22.44	14.33	8	14424	90238	29469857
Haematocrit decreased	22.39	14.33	46	14386	28976	29531119
Acinetobacter sepsis	22.28	14.33	5	14427	39	29560056
Thrombocytosis	22.13	14.33	16	14416	3337	29556758
Essential thrombocythaemia	22.05	14.33	5	14427	41	29560054
Squamous cell carcinoma	21.87	14.33	26	14406	10225	29549870
Capillary fragility	21.35	14.33	5	14427	48	29560047
Drug interaction	21.28	14.33	40	14392	197345	29362750
Leukoerythroblastosis	20.96	14.33	4	14428	12	29560083
Sickle cell disease	20.96	14.33	6	14426	133	29559962
Gangrene	20.96	14.33	17	14415	4201	29555894
Stenotrophomonas infection	20.78	14.33	12	14420	1705	29558390
Marrow hyperplasia	20.78	14.33	10	14422	981	29559114
Toxic epidermal necrolysis	20.61	14.33	34	14398	18119	29541976
Anaemia vitamin B12 deficiency	20.50	14.33	7	14425	281	29559814
Chronic myeloid leukaemia transformation	20.36	14.33	6	14426	148	29559947
Gene mutation	20.31	14.33	10	14422	1031	29559064
Malignant neoplasm progression	19.90	14.33	80	14352	73779	29486316
Erdheim-Chester disease	19.88	14.33	3	14429	0	29560095
Chronic myeloid leukaemia recurrent	19.53	14.33	6	14426	171	29559924
Pancytopenia	19.24	14.33	86	14346	83082	29477013
Pneumatosis	18.31	14.33	7	14425	390	29559705
Blood uric acid increased	18.22	14.33	18	14414	5750	29554345
Hip deformity	18.10	14.33	5	14427	97	29559998
Nasal polyps	17.86	14.33	11	14421	1758	29558337
Leukostasis syndrome	17.73	14.33	4	14428	32	29560063
Transformation to acute myeloid leukaemia	17.63	14.33	8	14424	687	29559408
Drug hypersensitivity	17.11	14.33	6	14426	68400	29491695
Bone marrow disorder	16.57	14.33	10	14422	1542	29558553
Spermatozoa morphology abnormal	16.27	14.33	3	14429	7	29560088
Anaemia macrocytic	16.12	14.33	12	14420	2616	29557479
Hypersplenism	15.98	14.33	6	14426	318	29559777
Differential white blood cell count abnormal	15.71	14.33	9	14423	1260	29558835
Night sweats	15.67	14.33	27	14405	14905	29545190
Neoplasm skin	15.64	14.33	7	14425	582	29559513
Squamous cell carcinoma of skin	15.39	14.33	21	14411	9465	29550630
Myocardial infarction	15.08	14.33	19	14413	110277	29449818
Myelodysplastic syndrome transformation	14.81	14.33	6	14426	390	29559705
Leukaemic infiltration pulmonary	14.68	14.33	3	14429	14	29560081
Febrile neutropenia	14.44	14.33	99	14333	112141	29447954
Amyotrophy	14.40	14.33	6	14426	419	29559676

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
Sickle cell anaemia with crisis	548.72	12.97	161	23928	5171	64469472
Acute myeloid leukaemia	252.37	12.97	146	23943	27317	64447326
Differentiation syndrome	198.05	12.97	59	24030	1995	64472648
Platelet count increased	186.79	12.97	105	23984	18591	64456052
Blast crisis in myelogenous leukaemia	165.59	12.97	42	24047	767	64473876
Myelofibrosis	156.45	12.97	50	24039	2143	64472500
Splenomegaly	153.14	12.97	91	23998	17870	64456773
Thrombocytopenia	141.67	12.97	279	23810	223522	64251121
White blood cell count increased	133.32	12.97	143	23946	65871	64408772
Chronic myeloid leukaemia	131.68	12.97	49	24040	3325	64471318
Tumour lysis syndrome	124.17	12.97	82	24007	19358	64455285
Acute chest syndrome	122.73	12.97	34	24055	882	64473761
Anaemia	112.24	12.97	353	23736	378327	64096316
Leukocytosis	104.34	12.97	97	23992	37643	64437000
Haemoglobin decreased	103.20	12.97	226	23863	194837	64279806
Philadelphia chromosome positive	97.12	12.97	26	24063	591	64474052
Platelet count decreased	88.32	12.97	194	23895	167517	64307126
Pancytopenia	84.96	12.97	174	23915	143135	64331508
Skin ulcer	83.07	12.97	92	23997	43882	64430761
Thrombocytosis	81.96	12.97	44	24045	7112	64467531
Hyperleukocytosis	77.32	12.97	29	24060	2011	64472632
Intentional product use issue	76.73	12.97	132	23957	95232	64379411
Myeloproliferative neoplasm	74.82	12.97	23	24066	866	64473777
Serum ferritin increased	69.82	12.97	42	24047	8426	64466217
Cytogenetic analysis abnormal	64.40	12.97	21	24068	960	64473683
Toxicity to various agents	63.80	12.97	28	24061	363485	64111158
Drug resistance	60.44	12.97	70	24019	35032	64439611
Febrile neutropenia	59.18	12.97	179	23910	187478	64287165
Squamous cell carcinoma	57.50	12.97	45	24044	13824	64460819
Blood lactate dehydrogenase increased	53.68	12.97	64	24025	33014	64441629
Completed suicide	52.67	12.97	10	24079	224404	64250239
Transformation to acute myeloid leukaemia	50.78	12.97	17	24072	844	64473799
Erythromelalgia	49.70	12.97	12	24077	177	64474466
Endocarditis noninfective	48.91	12.97	12	24077	190	64474453
Actinic keratosis	48.85	12.97	28	24061	5137	64469506
Posterior reversible encephalopathy syndrome	48.57	12.97	51	24038	22895	64451748
Granulomatous rosacea	48.50	12.97	12	24077	197	64474446
Pleural effusion	43.96	12.97	125	23964	126434	64348209
Drug hypersensitivity	43.82	12.97	17	24072	237798	64236845
Blast cell count increased	40.67	12.97	16	24073	1263	64473380
Malignant neoplasm progression	38.72	12.97	111	23978	112760	64361883
Drug abuse	38.08	12.97	3	24086	132371	64342272
Angiokeratoma	37.88	12.97	10	24079	215	64474428
Chronic myeloid leukaemia transformation	37.16	12.97	10	24079	232	64474411
Joint swelling	37.10	12.97	17	24072	215365	64259278
Gene mutation	36.22	12.97	17	24072	2065	64472578
Essential thrombocythaemia	36.14	12.97	9	24080	152	64474491
Mucosal inflammation	35.87	12.97	75	24014	62509	64412134
Idiopathic intracranial hypertension	35.58	12.97	18	24071	2575	64472068
Nail pigmentation	34.96	12.97	10	24079	292	64474351
Splenic infarction	34.45	12.97	19	24070	3238	64471405
Pyrexia	34.05	12.97	338	23751	558306	63916337
Haematocrit increased	33.97	12.97	19	24070	3326	64471317
Graft versus host disease in skin	32.79	12.97	22	24067	5325	64469318
Laryngitis	31.73	12.97	29	24060	11002	64463641
Infusion related reaction	31.56	12.97	11	24078	164456	64310187
Injection site pain	30.75	12.97	3	24086	111405	64363238
Leukostasis syndrome	30.72	12.97	7	24082	79	64474564
Chronic myelomonocytic leukaemia	29.59	12.97	11	24078	744	64473899
Neoplasm malignant	29.42	12.97	41	24048	24647	64449996
Arthropathy	29.21	12.97	5	24084	120962	64353681
Anaemia macrocytic	29.16	12.97	19	24070	4379	64470264
Cytomegalovirus infection reactivation	29.02	12.97	21	24068	5735	64468908
Red blood cell count decreased	28.92	12.97	59	24030	48327	64426316
Neutropenic colitis	28.46	12.97	19	24070	4562	64470081
Blood bilirubin increased	27.36	12.97	64	24025	57489	64417154
Hypersplenism	27.25	12.97	9	24080	428	64474215
Contraindicated product administered	27.06	12.97	4	24085	107825	64366818
Leukaemia	26.65	12.97	19	24070	5069	64469574
Antineutrophil cytoplasmic antibody positive	26.46	12.97	11	24078	1001	64473642
Blood iron increased	26.32	12.97	12	24077	1365	64473278
Bone marrow failure	25.78	12.97	56	24033	47896	64426747
Sickle cell anaemia	24.43	12.97	9	24080	593	64474050
Squamous cell carcinoma of skin	24.43	12.97	26	24063	11850	64462793
Haematocrit decreased	24.07	12.97	59	24030	54596	64420047
Haemoglobin increased	24.02	12.97	18	24071	5183	64469460
Rhabdomyolysis	23.97	12.97	3	24086	91723	64382920
Tongue neoplasm malignant stage unspecified	23.95	12.97	10	24079	920	64473723
Therapeutic product effect decreased	23.39	12.97	7	24082	115344	64359299
Electrocardiogram QT prolonged	23.34	12.97	74	24015	79374	64395269
Marrow hyperplasia	23.16	12.97	11	24078	1373	64473270
White blood cell count decreased	22.92	12.97	118	23971	157719	64316924
Sinusitis	22.90	12.97	13	24076	145915	64328728
Immunodeficiency	22.62	12.97	29	24060	16095	64458548
Acinetobacter sepsis	21.98	12.97	5	24084	56	64474587
Myelodysplastic syndrome	21.92	12.97	38	24051	27541	64447102
Leukaemia recurrent	21.73	12.97	13	24076	2581	64472062
Subacute combined cord degeneration	21.24	12.97	7	24082	331	64474312
Graft versus host disease	21.22	12.97	26	24063	13787	64460856
Parainfluenzae virus infection	20.99	12.97	16	24073	4727	64469916
Tyrosine kinase mutation	20.58	12.97	4	24085	19	64474624
Laryngeal inflammation	20.48	12.97	6	24083	191	64474452
Leukaemic infiltration pulmonary	20.41	12.97	4	24085	20	64474623
Second primary malignancy	20.22	12.97	24	24065	12313	64462330
Acute respiratory failure	20.00	12.97	52	24037	49882	64424761
Post cardiac arrest syndrome	19.80	12.97	4	24085	24	64474619
Erythropoiesis abnormal	19.43	12.97	7	24082	433	64474210
Adenocarcinoma metastatic	19.42	12.97	5	24084	97	64474546
Acute febrile neutrophilic dermatosis	18.76	12.97	13	24076	3316	64471327
Full blood count abnormal	18.63	12.97	37	24052	29720	64444923
Gangrene	18.63	12.97	18	24071	7320	64467323
Polycythaemia vera	18.62	12.97	6	24083	264	64474379
Platelet count abnormal	18.48	12.97	14	24075	4098	64470545
Acute myeloid leukaemia recurrent	18.39	12.97	12	24077	2772	64471871
Death	18.30	12.97	267	23822	482438	63992205
Therapy non-responder	18.11	12.97	60	24029	65839	64408804
Musculoskeletal stiffness	17.91	12.97	12	24077	123194	64351449
Tonsillitis bacterial	17.48	12.97	5	24084	146	64474497
Anaemia vitamin B12 deficiency	17.47	12.97	7	24082	580	64474063
Erdheim-Chester disease	17.39	12.97	3	24086	6	64474637
Stenotrophomonas infection	17.29	12.97	12	24077	3068	64471575
Disease progression	17.25	12.97	101	23988	141579	64333064
Pericardial effusion	16.88	12.97	42	24047	39212	64435431
Disseminated intravascular coagulation	16.51	12.97	37	24052	32311	64442332
Interstitial lung disease	16.27	12.97	76	24013	97656	64376987
Hip deformity	16.19	12.97	5	24084	191	64474452
Cytopenia	15.96	12.97	24	24065	15447	64459196
Retinopathy sickle cell	15.93	12.97	4	24085	70	64474573
Capillary fragility	15.83	12.97	5	24084	206	64474437
Blood pressure increased	15.80	12.97	25	24064	172527	64302116
Splenic rupture	15.74	12.97	10	24079	2209	64472434
Haemorrhage	15.71	12.97	65	24024	79286	64395357
Nasopharyngitis	15.62	12.97	31	24058	196042	64278601
Chromosome analysis abnormal	15.54	12.97	5	24084	219	64474424
Product use in unapproved indication	15.50	12.97	116	23973	176502	64298141
Cerebral haemorrhage	15.38	12.97	48	24041	51042	64423601
Subdural haemorrhage	15.36	12.97	14	24075	5289	64469354
Myeloblast count increased	15.31	12.97	3	24086	15	64474628
Hypercreatininaemia	15.25	12.97	7	24082	808	64473835
Pneumatosis	15.25	12.97	7	24082	809	64473834
Transplant failure	15.06	12.97	12	24077	3782	64470861
Peripheral swelling	15.05	12.97	35	24054	209118	64265525
Acute erythroid leukaemia	15.02	12.97	5	24084	244	64474399
Differential white blood cell count abnormal	14.98	12.97	9	24080	1801	64472842
Glossodynia	14.91	12.97	3	24086	64693	64409950
Rheumatoid arthritis	14.86	12.97	24	24065	164270	64310373
Hypersensitivity	14.85	12.97	32	24057	196420	64278223
Ovarian failure	14.51	12.97	6	24083	539	64474104
Gastroenteritis staphylococcal	14.44	12.97	5	24084	275	64474368
Insomnia	14.32	12.97	33	24056	197803	64276840
B-cell small lymphocytic lymphoma	14.32	12.97	4	24085	107	64474536
Cholestasis	14.29	12.97	43	24046	44829	64429814
Intentional overdose	14.13	12.97	8	24081	89936	64384707
Jaundice	14.07	12.97	45	24044	48467	64426176
Amyotrophy	14.04	12.97	6	24083	585	64474058
Tremor	14.03	12.97	21	24068	148209	64326434
Lactic acidosis	13.84	12.97	3	24086	61407	64413236
Maternal exposure before pregnancy	13.79	12.97	11	24078	3472	64471171
Venous pressure increased	13.78	12.97	3	24086	27	64474616
Extramedullary haemopoiesis	13.63	12.97	4	24085	128	64474515
Blood uric acid increased	13.58	12.97	16	24073	8147	64466496
Sickle cell disease	13.52	12.97	4	24085	132	64474511
Periarticular disorder	13.41	12.97	3	24086	31	64474612
Adenovirus infection	13.38	12.97	15	24074	7240	64467403
Acute leukaemia	13.36	12.97	8	24081	1590	64473053
Azoospermia	13.16	12.97	4	24085	145	64474498
Swelling	13.04	12.97	25	24064	160193	64314450
Early satiety	13.03	12.97	7	24082	1132	64473511
Chloroma	13.02	12.97	6	24083	699	64473944
Left ventricular dysfunction	13.01	12.97	23	24066	16931	64457712

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01XX05	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Other antineoplastic agents
FDA CS	M0022315	Urea
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D000986	Antisickling Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D006401	Hematologic Agents
MeSH PA	D019384	Nucleic Acid Synthesis Inhibitors
FDA EPC	N0000180853	Antimetabolite
CHEBI has role	CHEBI:35221	antimetabolite
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:48578	free radical scavengers
CHEBI has role	CHEBI:50846	Immunologic factor
CHEBI has role	CHEBI:50902	genotoxic agent
CHEBI has role	CHEBI:50905	teratogeno
CHEBI has role	CHEBI:59517	DNA synthesis inhibitors
CHEBI has role	CHEBI:64911	mitotic inhibitor
CHEBI has role	CHEBI:74213	EC 1.17.4.1 inhibitor

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

Disease	Relation	SNOMED_ID	DOID
Chronic myeloid leukemia	indication	92818009	DOID:8552
Hb SS disease	indication	127040003	DOID:10923
Malignant tumor of head and/or neck	indication	255056009
Malignant tumor of ovary	indication	363443007	DOID:2394
Malignant melanoma	indication	372244006
Hemoglobin SS disease with crisis	indication	417425009
Polycythemia vera	off-label use	109992005
Essential thrombocythemia	off-label use	109994006	DOID:2224
Vasculitis of the skin	contraindication	53312001
Leukopenia	contraindication	84828003	DOID:615
Kidney disease	contraindication	90708001	DOID:557
Anemia	contraindication	271737000	DOID:2355
Pregnancy, function	contraindication	289908002
Thrombocytopenic disorder	contraindication	302215000	DOID:1588
Breastfeeding (mother)	contraindication	413712001
Postirradiation Erythema	contraindication
Severe Bone Marrow Depression	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.38	acidic
pKa2	12.5	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
100MG	SIKLOS	ADDMEDICA SAS	N208843	Dec. 21, 2017	RX	TABLET	ORAL	Dec. 21, 2024	TO REDUCE THE FREQUENCY OF PAINFUL CRISES AND TO REDUCE THE NEED FOR BLOOD TRANSFUSIONS IN PEDIATRIC PATIENTS, 2 YEARS OF AGE AND OLDER, WITH SICKLE CELL ANEMIA WITH RECURRENT MODERATE TO SEVERE PAINFUL CRISIS
1GM	SIKLOS	ADDMEDICA SAS	N208843	Dec. 21, 2017	RX	TABLET	ORAL	Dec. 21, 2024	TO REDUCE THE FREQUENCY OF PAINFUL CRISES AND TO REDUCE THE NEED FOR BLOOD TRANSFUSIONS IN PEDIATRIC PATIENTS, 2 YEARS OF AGE AND OLDER, WITH SICKLE CELL ANEMIA WITH RECURRENT MODERATE TO SEVERE PAINFUL CRISIS

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Ribonucleoside-diphosphate reductase large subunit	Enzyme	P23921	RIR1_HUMAN	INHIBITOR			WOMBAT-PK	CHEMBL
Ribonucleoside-diphosphate reductase subunit M2	Enzyme	P31350	RIR2_HUMAN	INHIBITOR			WOMBAT-PK	CHEMBL
Carbonic anhydrase 2	Enzyme	P00918	CAH2_HUMAN		Ki	4.55	CHEMBL
Carbonic anhydrase 9	Enzyme	Q16790	CAH9_HUMAN		Ki	4.64	CHEMBL
Carbonic anhydrase 5A, mitochondrial	Enzyme	P35218	CAH5A_HUMAN		Ki	4.51	CHEMBL

External reference:

ID	Source
4017733	VUID
N0000146101	NUI
D00341	KEGG_DRUG
4017733	VANDF
CHEBI:44423	CHEBI
NHY	PDB_CHEM_ID
CHEMBL467	ChEMBL_ID
6822	IUPHAR_LIGAND_ID
DB01005	DRUGBANK_ID
X6Q56QN5QC	UNII
3657	PUBCHEM_CID
1999309	RXNORM
148307	MMSL
1763	MMSL
4856	MMSL
d01373	MMSL
002635	NDDF
387314007	SNOMEDCT_US
56602009	SNOMEDCT_US
D006918	MESH_DESCRIPTOR_UI
C0020402	UMLSCUI
1991	INN_ID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
HYDREA	HUMAN PRESCRIPTION DRUG LABEL	1	0003-0830	CAPSULE	500 mg	ORAL	NDA	27 sections
DROXIA	HUMAN PRESCRIPTION DRUG LABEL	1	0003-6335	CAPSULE	200 mg	ORAL	NDA	29 sections
DROXIA	HUMAN PRESCRIPTION DRUG LABEL	1	0003-6336	CAPSULE	300 mg	ORAL	NDA	29 sections
DROXIA	HUMAN PRESCRIPTION DRUG LABEL	1	0003-6337	CAPSULE	400 mg	ORAL	NDA	29 sections
HYDROXYUREA	HUMAN PRESCRIPTION DRUG LABEL	1	0555-0882	CAPSULE	500 mg	ORAL	ANDA	23 sections
HYDROXYUREA	HUMAN PRESCRIPTION DRUG LABEL	1	0555-0882	CAPSULE	500 mg	ORAL	ANDA	23 sections
Hydroxyurea	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6939	CAPSULE	500 mg	ORAL	ANDA	24 sections
Hydroxyurea	HUMAN PRESCRIPTION DRUG LABEL	1	10135-702	CAPSULE	500 mg	ORAL	ANDA	30 sections
HYDROXYUREA	HUMAN PRESCRIPTION DRUG LABEL	1	42291-321	CAPSULE	500 mg	ORAL	ANDA	22 sections
Hydroxyurea	HUMAN PRESCRIPTION DRUG LABEL	1	49884-724	CAPSULE	500 mg	ORAL	ANDA	23 sections
HYDROXYUREA	HUMAN PRESCRIPTION DRUG LABEL	1	54868-4773	CAPSULE	500 mg	ORAL	ANDA	19 sections
Hydroxyurea	HUMAN PRESCRIPTION DRUG LABEL	1	55154-3554	CAPSULE	500 mg	ORAL	ANDA	24 sections
Hydroxyurea	HUMAN PRESCRIPTION DRUG LABEL	1	55154-7143	CAPSULE	500 mg	ORAL	ANDA	26 sections
Hydroxyurea	HUMAN PRESCRIPTION DRUG LABEL	1	60429-265	CAPSULE	500 mg	ORAL	ANDA	23 sections
Hydroxyurea	HUMAN PRESCRIPTION DRUG LABEL	1	68084-284	CAPSULE	500 mg	ORAL	ANDA	26 sections
HYDROXYUREA	HUMAN PRESCRIPTION DRUG LABEL	1	69315-164	CAPSULE	500 mg	ORAL	ANDA	17 sections
Hydroxyurea	HUMAN PRESCRIPTION DRUG LABEL	1	70518-0916	CAPSULE	500 mg	ORAL	ANDA	23 sections
Siklos	HUMAN PRESCRIPTION DRUG LABEL	1	71770-100	TABLET, FILM COATED	100 mg	ORAL	NDA	35 sections
Siklos	HUMAN PRESCRIPTION DRUG LABEL	1	71770-105	TABLET, FILM COATED	100 mg	ORAL	NDA	35 sections
Siklos	HUMAN PRESCRIPTION DRUG LABEL	1	71770-105	TABLET, FILM COATED	100 mg	ORAL	NDA	35 sections
Siklos	HUMAN PRESCRIPTION DRUG LABEL	1	71770-120	TABLET, FILM COATED	1000 mg	ORAL	NDA	35 sections
Siklos	HUMAN PRESCRIPTION DRUG LABEL	1	71770-120	TABLET, FILM COATED	1000 mg	ORAL	NDA	35 sections