Hydralazine

Summary

Hydralazine (CHEMBL276832) is an approved small-molecule antihypertensive agent (ATC C02DB02); indicated across 20 conditions including hypertensive disorder and atherosclerosis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C02DB02
• Indications: 20 conditions
• Clinical trials: 34
• Chemistry: 160.18 Da · C8H8N4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL276832
Name	Hydralazine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	3637
ChEBI	CHEBI:5775
ATC	C02DB02
Molecular formula	C8H8N4
Molecular weight	160.18
InChIKey	RPTUSVTUFVMDQK-UHFFFAOYSA-N

SMILES: C1=CC=C2C(=C1)C=NN=C2NN

IUPAC name: phthalazin-1-ylhydrazine

ChEBI definition: The 1-hydrazino derivative of phthalazine; a direct-acting vasodilator that is used as an antihypertensive agent.

Pharmacological roles (ChEBI): antihypertensive agent, vasodilator agent.

Also known as: Hidralazina, Hydralazine, Hydralazine polistirex, NSC-126699, hydralazine, SID11111261, SID11111262, SID90341825, SID50111090, HYDRALAZINE, SID174006923

Parent form; salt/anhydrous children: CHEMBL542541

Patent coverage: 6,635 distinct patent families (23,794 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 23,781 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 26 (assay-derived). Sample: Pyruvate kinase PKM, Lysine-specific demethylase 4E, Nuclear receptor ROR-gamma, Survival motor neuron protein, Fructose-bisphosphate aldolase, Prelamin-A/C, 4’-phosphopantetheinyl transferase ffp, Thrombopoietin, NPC intracellular cholesterol transporter 1, Ras-related protein Rab-9A.

Bioactivity

ChEMBL activities: 32 potent at pChembl ≥ 5 of 44 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P08482	7.55	Potency	28.2	nM	CHEMBL_ACT_4807527
THPO	7.4	Potency	39.8	nM	CHEMBL_ACT_4809550
THPO	7.4	Potency	39.8	nM	CHEMBL_ACT_5074257
ACOX1	6.38	IC50	420	nM	CHEMBL_ACT_25097936
MPO	6.05	IC50	900	nM	CHEMBL_ACT_16843813
MPO	6.05	IC50	900	nM	CHEMBL_ACT_16843816
MPO	6.05	IC50	900	nM	CHEMBL_ACT_18064398
CYP1A2	6	AC50	1000	nM	CHEMBL_ACT_6067973
P80025	5.92	IC50	1200	nM	CHEMBL_ACT_18064501
TP53	5.8	Potency	1585	nM	CHEMBL_ACT_4862262
Q27686	5.7	Potency	1995	nM	CHEMBL_ACT_3692487
Q27686	5.7	Potency	1995	nM	CHEMBL_ACT_3701115
RAB9A	5.64	Potency	2311	nM	CHEMBL_ACT_3856119
MPO	5.63	IC50	2360	nM	CHEMBL_ACT_18064453
TP53	5.6	Potency	2512	nM	CHEMBL_ACT_4838212
TP53	5.6	Potency	2512	nM	CHEMBL_ACT_4846956
NPC1	5.59	Potency	2593	nM	CHEMBL_ACT_4748626
LMNA	5.5	Potency	3162	nM	CHEMBL_ACT_3642002
CYP1A2	5.5	AC50	3162	nM	CHEMBL_ACT_6007579
P12530	5.44	IC50	3649	nM	CHEMBL_ACT_7666607
AOX1	5.41	IC50	3930	nM	CHEMBL_ACT_19342743
SMN1	5.4	Potency	3981	nM	CHEMBL_ACT_3878540
P08659	5.4	Potency	3981	nM	CHEMBL_ACT_3950669
TP53	5.4	Potency	3981	nM	CHEMBL_ACT_4862795
CYP3A4	5.4	Potency	3981	nM	CHEMBL_ACT_4973740
CYP3A4	5.4	Potency	3981	nM	CHEMBL_ACT_5042766
CYP3A4	5.4	AC50	3981	nM	CHEMBL_ACT_6065795
ALDH1A1	5.3	Potency	5012	nM	CHEMBL_ACT_4177243
Q9F4F7	5.3	Potency	5012	nM	CHEMBL_ACT_4373079
PTGS1	5.21	AC50	6184	nM	CHEMBL_ACT_25206362

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

20 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
hypertensive disorder	4	MONDO:0005044	EFO:0000537
atherosclerosis	3	MONDO:0005311	EFO:0003914
ovarian cancer	3	MONDO:0008170	MONDO:0008170
coronary artery disorder	3	MONDO:0005010	EFO:0001645
type 2 diabetes mellitus	3	MONDO:0005148	MONDO:0005148
congestive heart failure	2	MONDO:0005009	EFO:0000373
neoplasm	2	MONDO:0005070	EFO:0000616
preeclampsia	2	MONDO:0005081	EFO:0000668
heart disorder	2	MONDO:0005267	EFO:0003777
intracerebral hemorrhage	2	MONDO:0013792	EFO:0005669
stroke disorder	2	MONDO:0005098	EFO:0000712
breast neoplasm	2	MONDO:0021100	MONDO:0007254
cardiovascular disorder	2	MONDO:0004995	EFO:0000319
heart failure	2	MONDO:0005252	EFO:0003144
vascular disorder	2	MONDO:0005385	EFO:0004264
rectal cancer	1	MONDO:0006519	EFO:1000657
lung neoplasm	1	MONDO:0021117	MONDO:0008903
polycystic kidney disease	0	MONDO:0020642	EFO:0008620

2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 34.

Phase distribution

Phase	Trials
PHASE2	10
PHASE3	6
Not specified	6
PHASE4	4
PHASE1/PHASE2	3
PHASE1	3
PHASE2/PHASE3	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06218199	PHASE4	RECRUITING	Diuretics vs. Afterload Reduction for Treatment of HeartLogic Alerts
NCT00661895	PHASE4	COMPLETED	Black Education and Treatment of Hypertension (BEAT HTN)
NCT02046395	PHASE4	COMPLETED	Effect of Renin-angiotensin-system Blockade on Urinary Free Light Chains in Patients With Type 2 Diabetes Mellitus
NCT02228408	PHASE4	COMPLETED	Safety and Cardiovascular Efficacy of Hydralazine and Isosorbide Dinitrate in Dialysis-Dependent ESRD
NCT00532818	PHASE3	UNKNOWN	Hydralazine Valproate for Cervical Cancer
NCT00533299	PHASE3	UNKNOWN	Hydralazine Valproate for Ovarian Cancer
NCT01255475	PHASE2/PHASE3	COMPLETED	Blood Pressure Reduction in Heart Failure
NCT01538875	PHASE3	COMPLETED	Hydralazine Versus Labetalol for the Management of Hypertensive Disorders of Pregnancy
NCT01822808	PHASE3	UNKNOWN	Bi Treatment With Hydralazine/Nitrates Versus Placebo in Africans Admitted With Acute Heart Failure
NCT02343393	PHASE3	UNKNOWN	Nitrates In Combination With Hydralazine in cardiorEnal Syndrome (NICHE) Study
NCT02446652	PHASE3	WITHDRAWN	Evaluation of TRANSKRIP ® Plus Chemotherapy in Recurrent-Persistent Cervical Cancer
NCT00000499	PHASE2	COMPLETED	Systolic Hypertension in the Elderly Program (SHEP) (Pilot Study)
NCT00395655	PHASE2	TERMINATED	Hydralazine and Valproate Added to Chemotherapy for Breast Cancer
NCT00404326	PHASE2	COMPLETED	Hydralazine and Valproate Plus Cisplatin Chemoradiation in Cervical Cancer
NCT00404508	PHASE2	COMPLETED	A Phase II Study of Epigenetic Therapy to Overcome Chemotherapy Resistance in Refractory Solid Tumors
NCT00575640	PHASE1/PHASE2	WITHDRAWN	Hydralazine as a Demethylating Agent in Rectal Cancer
NCT00575978	PHASE1/PHASE2	WITHDRAWN	Hydralazine as Demethylating Agent in Breast Cancer
NCT00963976	PHASE2	COMPLETED	Intracerebral Hemorrhage Acutely Decreasing Arterial Pressure Trial
NCT01516346	PHASE2	COMPLETED	Vasodilator Therapy for Heart Failure and Preserved Ejection Fraction
NCT02050529	PHASE2	COMPLETED	Randomized Controlled Trial of Labetalol Versus Hydralazine for Severe Hypertension in Obstetric Patients.
NCT02281838	PHASE2	TERMINATED	The Intracerebral Hemorrhage Acutely Decreasing Arterial Pressure Trial II
NCT04116112	PHASE2	COMPLETED	Blood Pressure After Endovascular Stroke Therapy-II
NCT04484350	PHASE2	COMPLETED	Blood Pressure Management in Stroke Following Endovascular Treatment
NCT06360601	PHASE1/PHASE2	UNKNOWN	Intravenous Labetalol Versus Hydralazine in Preeclampsia
NCT00223717	PHASE1	COMPLETED	Treatment of Supine Hypertension in Autonomic Failure
NCT00996060	PHASE1	COMPLETED	Use of Hydralazine and Valproic Acid in Advanced Solid Tumor Malignancies
NCT01587313	PHASE1	COMPLETED	A Comparison of Various Combinations of BiDil Capsules and BiDil Tablets in Healthy Human Volunteers
NCT03423810	EARLY_PHASE1	COMPLETED	Assessing a Dose-Response Relationship of Hydralazine and Its Effects on DNA Methyltransferase 1 in Polycystic Kidney Disease Patients
NCT00204984	Not specified	COMPLETED	Heart and Blood Pressure Study: The Effect of Aortic Impedance on Myocardial Relaxation
NCT00599235	Not specified	COMPLETED	Sildenafil and Exercise Capacity in Hypertension
NCT00607477	Not specified	TERMINATED	Pilot Study of the Treatment of Vascular Endothelial Growth Factor(VEGF)Signaling Pathway Inhibitor-Induced Hypertension
NCT02933593	Not specified	WITHDRAWN	Changes in Central Arterial Pressure When Comparing ACOG Hypertensive Urgency Protocols
NCT04435210	Not specified	COMPLETED	Efficacy of Nifedipine Versus Hydralazine in Management of Severe Hypertension in Pregnancy
NCT07572656	Not specified	COMPLETED	Comparison of Intravenous Labetalol and Intravenous Hydralazine in Severe Preeclampsia

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (1) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of CPIC Guideline for hydralazine and NAT2	CPIC	NAT2	yes	yes

PharmGKB also curates 3 clinical and 34 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).