THERAPY DOSSIER · th-f0b433b4519b

Alpha-adrenoceptor antagonists: phentolamine (non-selective), prazosin and silodosin (alpha-1 selective) and yohimbine (alpha-2 selective)

Drug · PARTIAL identity match: the ChEMBL record covers the PHENTOLAMINE component ONLY. CHEMBL597 is the parent of CHEMBL1200873 (phentolamine mesylate), max_phase 4, first approval 1952, ATC C04AB01 and V03AB36, no black box warning, not withdrawn. Mechanism (mec_id 1236, held against the mesylate) is adrenergic receptor alpha ANTAGONIST, direct_interaction true, disease_efficacy true, target CHEMBL2095203. Prazosin, silodosin and yohimbine were NOT separately queried within the time budget, so this entry is incomplete by OMISSION for those three agents. NCT00104104 (zoledronic acid in myeloma) was returned by the query and REJECTED as an irrelevant match.

No trauma translation Suggest a correction

This record is classified as “NO TRAUMA TRANSLATION”. Read the indication and notes below for the specific context.

Evidence & regulatory context

Mechanism: PARTIAL identity match: the ChEMBL record covers the PHENTOLAMINE component ONLY. CHEMBL597 is the parent of CHEMBL1200873 (phentolamine mesylate), max_phase 4, first approval 1952, ATC C04AB01 and V03AB36, no black box warning, not withdrawn. Mechanism (mec_id 1236, held against the mesylate) is adrenergic receptor alpha ANTAGONIST, direct_interaction true, disease_efficacy true, target CHEMBL2095203. Prazosin, silodosin and yohimbine were NOT separately queried within the time budget, so this entry is incomplete by OMISSION for those three agents. NCT00104104 (zoledronic acid in myeloma) was returned by the query and REJECTED as an irrelevant match.
Target: CHEMBL2095203
Injury models: Other
Reported indication: Not recorded
First approval: 1952
Development stage: Not recorded
ChEMBL record: CHEMBL597 ↗
ChEMBL max phase: 4 / 4 (development scale, not regulatory approval)
Synonyms: Fentolamina; Phentolamin; Phentolamine; Phentolamine mesylate (CHEMBL1200873); Oraverse; Regitine; Rogitine; Ryzumvi; NV-101
Note: Not recorded

Clinical trials 9

0 linked trials carry an injury-indication flag. These flags support record-level exploration and sit alongside the stringent aggregate counts described in Methods.

NCT05687669 ↗PHASE4completed

Phentolamine versus glyceryl trinitrate and renal function in pre-eclampsia patients in ICU

Pre-Eclampsia; Complicating Pregnancy

Enrolment: 170 · Results not recorded

NCT05223478 ↗PHASE3completed

Nyxol (0.75% phentolamine ophthalmic solution) to reverse pharmacologically induced mydriasis in healthy pediatric subjects

Mydriasis · Dilation

Enrolment: 23 · Results not recorded

NCT05134974 ↗PHASE3completed

Nyxol (0.75% phentolamine ophthalmic solution) to reverse pharmacologically-induced mydriasis in healthy subjects

Mydriasis · Dilation

Enrolment: 368 · Results not recorded

NCT00309361 ↗PHASE3completed

NV-101 (phentolamine mesylate) in dental patients undergoing mandibular procedures

Anesthesia, Dental

Enrolment: 240 · Results not recorded

NCT03960866 ↗PHASE2completed

Phentolamine mesylate ophthalmic solution in subjects with open angle glaucoma or ocular hypertension

Open Angle Glaucoma · Ocular Hypertension

Enrolment: 39 · Results not recorded

NCT03318094 ↗PHASE1active not recruiting

Phentolamine, saline and sodium nitroprusside in insulin resistance, obesity and healthy volunteers

Insulin Resistance · Healthy · Obesity

Enrolment: 36 · Results not recorded

NCT04110808 ↗EARLY_PHASE1unknown

Hypotensive anaesthesia using nitroglycerine versus phentolamine on event related potentials and cognitive function in septoplasty

Effect of Drugs

Enrolment: 60 · Results not recorded

NCT05219799 ↗EARLY_PHASE1recruiting

Sex disparities in hypoxic vasodilation and impact of obesity (phentolamine mesylate, propranolol, isoproterenol, norepinephrine)

Obesity · Vasodilation · Healthy

Enrolment: 72 · Results not recorded

NCT06787066 ↗EARLY_PHASE1recruiting

Sympathetic vascular transduction across the menopause transition (propranolol, phentolamine injection)

Menopause

Enrolment: 75 · Results not recorded

Preclinical evidence 1

1 studies reported at therapy level; 1 evidence entries itemised.

PMID 26492290 ↗2015Mixed findings

Attenuation of pain behaviour by local administration of alpha-2 adrenoceptor antagonists to dorsal root ganglia in a rat radiculopathy model.

RatOtherSprague-DawleyMalen = 130 male Sprague-Dawley rats in totalLocal injection around the dorsal root ganglionThree consecutive daily injections starting on day 0, day 4 or day 11 after roo…

Model: Nerve root constriction radiculopathy model

Phentolamine and yohimbine given from day 0 continually attenuated pain behaviour, high dose prazosin attenuated pain behaviour whereas low dose prazosin did not, and silodosin had no analgesic effect. Phentolamine started on day 4 attenuated established pain behaviour up to postoperative day 28 al…

Extraction: extract · Supplied extraction confidence: 0.7. Machine-extracted fields require source verification.

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Alpha-adrenoceptor antagonists: phentolamine (non-selective), prazosin and silodosin (alpha-1 selective) and yohimbine (alpha-2 selective)