Isoflurane

Summary

Isoflurane (CHEMBL1256) is an approved small-molecule inhalation anaesthetic (ATC N01AB06) targeting TRPA1, KCNK2, and KCNK3; indicated across 8 conditions including severe acute respiratory syndrome and respiratory failure.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N01AB06
• Targets: 4 (TRPA1, KCNK2, KCNK3…)
• Indications: 8 conditions
• Clinical trials: 75
• Chemistry: 184.49 Da · C3H2ClF5O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1256
Name	Isoflurane
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	3763
ChEBI	CHEBI:6015
ATC	N01AB06
Molecular formula	C3H2ClF5O
Molecular weight	184.49
InChIKey	PIWKPBJCKXDKJR-UHFFFAOYSA-N

SMILES: C(C(F)(F)F)(OC(F)F)Cl

IUPAC name: 2-chloro-2-(difluoromethoxy)-1,1,1-trifluoroethane

Pharmacological roles (ChEBI): inhalation anaesthetic.

Also known as: Aerrane, COMPOUND 469, COMPOUND-469, Forane, Isoflurane, Isoflurano, SID50125772, ISOFLURANE, isoflurane, SID144206238, SID144208029

Patent coverage: 35,331 distinct patent families (114,067 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
TRPA1	TRPA1	Activation	3.7	0.1%	O75762
KCNK2	K2P2.1			0.2%	O95069
KCNK3	K2P3.1	Positive	2.7	0%	O14649
KCNK16	K2P16.1			0%	Q96T55

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Menin/Histone-lysine N-methyltransferase MLL.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 4 target gene(s): TRPA1, KCNK2, KCNK3, KCNK16.

Top Reactome pathways

10 total, by targets touching each:

Pathway	Targets	Genes
Neuronal System	3	KCNK16, KCNK2, KCNK3
Potassium Channels	3	KCNK16, KCNK2, KCNK3
Tandem pore domain potassium channels	3	KCNK16, KCNK2, KCNK3
Muscle contraction	3	KCNK16, KCNK2, KCNK3
Phase 4 - resting membrane potential	3	KCNK16, KCNK2, KCNK3
Cardiac conduction	3	KCNK16, KCNK2, KCNK3
TWIK-releated acid-sensitive K+ channel (TASK)	1	KCNK3
TWIK-related alkaline pH activated K+ channel (TALK)	1	KCNK16
TWIK related potassium channel (TREK)	1	KCNK2
TRP channels	1	TRPA1

Dominant GO biological processes

GO term	Targets
monoatomic ion transport	4
monoatomic ion transmembrane transport	4
potassium ion transmembrane transport	3
potassium ion transport	3
response to xenobiotic stimulus	2
cellular response to hypoxia	2
cochlea development	2
regulation of membrane potential	2
intracellular calcium ion homeostasis	1
cell surface receptor signaling pathway	1
response to cold	1
urinary bladder smooth muscle contraction	1
sensory perception of pain	1
cellular response to heat	1
positive regulation of insulin secretion involved in cellular response to glucose stimulus	1

Indications & clinical

Indications

7 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
severe acute respiratory syndrome	3	MONDO:0005091	MONDO:0100096
respiratory failure	3	MONDO:0021113	EFO:0009686
opiate dependence	2	MONDO:0005530	EFO:0005611
subarachnoid hemorrhage	2	MONDO:0005099	EFO:0000713
drug dependence	2	MONDO:0005303	EFO:0003890
acute respiratory distress syndrome	2	MONDO:0006502	EFO:1000637
heart disorder	1	MONDO:0005267	EFO:0003777

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

Clinical trials

Total trials: 75.

Phase distribution

Phase	Trials
Not specified	34
PHASE4	18
PHASE3	10
PHASE1	6
PHASE2	4
PHASE2/PHASE3	3

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07000526	PHASE4	RECRUITING	Inhaled Sedation in Critically Ill Patients
NCT07496593	PHASE4	ACTIVE_NOT_RECRUITING	Total Intravenous and Balanced Anesthesia in Diabetic Patients Undergoing Video-Assisted Thoracoscopy
NCT00244517	PHASE4	TERMINATED	DIAFAX I+II-Effects of Inhalative Anesthetics on Left Ventricular Diastolic Function
NCT00333632	PHASE4	WITHDRAWN	Effect of Dexmedetomidine Upon Sleep Postoperatively
NCT00575354	PHASE4	COMPLETED	Comparison of Sevoflurane and Isoflurane Anesthesia for Benign Breast Tumor Excision
NCT00830843	PHASE4	COMPLETED	Inhalatorial Sedation in Patient With Subarachnoid Hemorrhage (SAH) Versus Conventional Intravenous Sedation
NCT00922844	PHASE4	TERMINATED	The Effect of Sevoflurane Versus Isoflurane on Vasopressor Need
NCT01111227	PHASE4	COMPLETED	Inflammatory Cytokines Profile in Individuals Subjected to Surgical Procedures Using Propofol or Isoflurane
NCT01212523	PHASE4	COMPLETED	Effects of Propofol and Isoflurane on Pulmonary Vascular Resistance
NCT01397331	PHASE4	TERMINATED	Influence of Anesthesia on Mechanical Efficiency of Left Ventricle in Patients Undergoing Open Heart Surgery
NCT01601795	PHASE4	COMPLETED	Sevoflurane and Isoflurane - During Cardiopulmonary Bypass With the MECC System (Minimized Extracorporeal Circuit)
NCT02105610	PHASE4	COMPLETED	Volatile Anesthetics to Reduce Mortality in Cardiac Surgery
NCT02111447	PHASE4	TERMINATED	Post Anesthesia Emergence and Behavioral Changes in Children Undergoing MRI
NCT02154074	PHASE4	UNKNOWN	Dexmedetomidine Influence on the Level of Perioperative Blood Glucose and Insulin of Elderly Diabetes Patients
NCT02925611	PHASE4	COMPLETED	Comparison of Postoperative Delirium in Patients Anaesthetised With Isoflurane and Desflurane During Spinal Surgery
NCT03146104	PHASE4	COMPLETED	Comparison of Total Intravenous Anesthesia vs. Inhalational Anesthesia in Acute Subdural Hematoma Patients
NCT04039854	PHASE4	UNKNOWN	Comparison Between Propofol and Inhalational Anaesthetic Agents on Cardiovascular Outcomes Following Cardiac Surgery
NCT04074460	PHASE4	COMPLETED	Volatile Anaesthesia and Perioperative Outcomes Related to Cancer Feasibility Study
NCT04341350	PHASE3	RECRUITING	Comparison of an Inhaled Sedation Strategy to an Intravenous Sedation Strategy in Intensive Care Unit Patients Treated With Invasive Mechanical Ventilation
NCT06624592	PHASE3	RECRUITING	Sevoflurane/Dexmedetomidine vs. Isoflurane for Pediatric Emergence Delirium
NCT07099014	PHASE3	NOT_YET_RECRUITING	Inhaled Isoflurane for Sedation of Invasively Ventilated Patients With Cardiogenic Shock on Extracorporeal Membrane Oxygenation
NCT01406678	PHASE2/PHASE3	COMPLETED	Remote Ischemic Preconditioning in Coronary Artery Bypass Grafting With Cold Crystalloid Cardioplegic Arrest
NCT01839084	PHASE3	COMPLETED	PaNeX: Partial Nephrectomy Under Xenon
NCT02512809	PHASE3	TERMINATED	Isoflurane-induced Neuroinflammation in Children With Hydrocephalus
NCT03588429	PHASE3	COMPLETED	The Ratio of Hypnotic to Analgesic Potency of Volatile Anesthetics
NCT04684238	PHASE3	COMPLETED	Effect & Safety of Inhaled Isoflurane vs IV Midazolam for Sedation in Mechanically Ventilated Children 3-17 Years Old
NCT05312385	PHASE3	COMPLETED	Efficacy and Safety of Inhaled Isoflurane Delivered Via the Sedaconda ACD-S Compared to Intravenous Propofol for Sedation of Mechanically Ventilated Intensive Care Unit Adult Patients (INSPiRE-ICU1)
NCT05327296	PHASE3	COMPLETED	Efficacy and Safety of Inhaled Isoflurane Delivered Via the Sedaconda ACD-S Compared to Intravenous Propofol for Sedation of Mechanically Ventilated Intensive Care Unit Adult Patients (INSPiRE-ICU2)
NCT05696509	PHASE3	COMPLETED	Influence of Anesthetics on Clinical Outcome in Mitral and Aortic Valve Replacement in Adults
NCT06014138	PHASE2/PHASE3	UNKNOWN	Volatile Sedation for Patients With the Acute Respiratory Distress Syndrome
NCT06418893	PHASE2/PHASE3	UNKNOWN	Effect of TCI Propofol on Liver Transplant (TCI) Propofol on Intra-operative Usage of Vasopressors in Liver Transplant Recipients.
NCT00000251	PHASE2	COMPLETED	Effects of Subanesthetic Concentrations of Isoflurane/Nitrous Oxide - 3
NCT00000254	PHASE2	COMPLETED	Isoflurane at Subanesthetic Concentrations - 6
NCT03373266	PHASE2	COMPLETED	Serun Fluoride and Kidney Transplant
NCT04171193	PHASE2	UNKNOWN	Efficacy of Deep Anaesthesia With Isoflurane as a Fast-response Antidepressant Agent
NCT01302353	PHASE1	COMPLETED	Phase I Trial of Emulsified Isoflurane
NCT01640275	PHASE1	COMPLETED	Markers of Alzheimers Disease After Propofol or Isoflurane Anesthesia
NCT03569085	PHASE1	COMPLETED	Inhaled Anesthetics and Myocardial Strain
NCT05314569	PHASE1	COMPLETED	Cardioprotective Effect of Ketamine-dexmeditomidine Versus Fentanyl-midazolam in Open Heart Surgery in Pediatrics
NCT05695287	PHASE1	COMPLETED	The Effects of Sevoflurane, Isoflurane and Propofol During Cardiac Surgery
NCT05742789	PHASE1	COMPLETED	Effect of Anesthetics on Troponin I and С-reactive Protein
NCT06311604	Not specified	RECRUITING	Evaluation of the Safety of Inhaled Sedation With Isoflurane in Head Trauma Patients
NCT07152912	Not specified	RECRUITING	Impact of Isoflurane and Sevoflurane on Oxidative Stress in Patients Undergoing Laparoscopic Cholecystectomy
NCT07457593	Not specified	AVAILABLE	Expanded Access for Inhaled Isoflurane Delivered Via the Sedaconda ACD-S for Sedation of Difficult-to-Sedate Adult Mechanically Ventilated Intensive Care Unit Patients
NCT07460050	Not specified	NOT_YET_RECRUITING	Comparison of Two Sedative Agents in Terms of Controlled Hypotension
NCT07543523	Not specified	ACTIVE_NOT_RECRUITING	The Influence of Genetic Polymorphism on Dose- Dependent Analgesic Response and Safety to Propofol in General Anesthesia
NCT00434382	Not specified	UNKNOWN	Neuronal Mechanisms of Sensory Processing During General Anesthesia
NCT00521612	Not specified	COMPLETED	Sevoflurane vs. Isoflurane for Low-Flow General Anaesthesia for Abdominal Surgery
NCT00615472	Not specified	TERMINATED	Intravenous Versus Inhalational Anesthesia in Parkinson’s Disease
NCT00815269	Not specified	COMPLETED	Vasodilation Effect of Inhalational Anesthetics
NCT00983918	Not specified	COMPLETED	Pain After Laparoscopic Cholecystectomy
NCT01031550	Not specified	TERMINATED	Isoflurane Preconditioning for Liver Resections
NCT01151254	Not specified	COMPLETED	Comparison of Propofol Based Versus Volatile Based Anesthesia and Postoperative Sedation
NCT01171833	Not specified	COMPLETED	Ventilatory Effect on Speed of Anesthesia Under Various Inhaled Anesthetics
NCT01379664	Not specified	COMPLETED	Volatile Anesthetic Choice and Duration of Hospitalization: A Quality Improvement and Cost-control Project
NCT01512147	Not specified	COMPLETED	Dexmedetomidine on Intraoperative Somatosensory and Motor Evoked Potential Monitoring During Neurosurgery in Pediatric Patients
NCT01772537	Not specified	TERMINATED	The Effects of Anesthesia on Patients Undergoing Surgery for Repair of a Thoracoabdominal Aneurysm.
NCT01819012	Not specified	COMPLETED	Effect of Isoflurane on Tissue Doppler Imaging of Mitral Annulus During Cardiac Surgery
NCT01983800	Not specified	COMPLETED	AnaConDa Long Term Sedation Study
NCT02185118	Not specified	UNKNOWN	Effects of Subanesthetic Isoflurane/Sevoflurane in 60% Oxygen on Clinical In-vitro Experimental Sepsis
NCT02222142	Not specified	COMPLETED	Volatile Versus Propofol Anesthesia in OPCAB
NCT02326727	Not specified	UNKNOWN	Influence of Epidural Analgesia on Natural Killer Cell (NK) Activity After Colonic Cancer Surgery
NCT02342509	Not specified	COMPLETED	Automated Control of End-tidal Volatile Anesthetic Concentration
NCT02625181	Not specified	COMPLETED	Real-time Decision Support for Postoperative Nausea and Vomiting (PONV) Prophylaxis
NCT02726620	Not specified	COMPLETED	Decision Support for Intraoperative Low Blood Pressure
NCT02739958	Not specified	COMPLETED	Effects of Propofol-dexmedetomidine on Immune Function in Patients With Cancer Larynx
NCT03860129	Not specified	COMPLETED	Different Volatile Anaesthetics and the Depth of Long Term ICU Sedation
NCT03882788	Not specified	COMPLETED	The Effect of Anesthesia on Neurodevelopmental Outcome (NDO)
NCT04188314	Not specified	COMPLETED	Comparing Quality of Recovery Between Desflurane & Isoflurane in Eye Surgery Patients at Dr George Mukhari Acad Hospital
NCT05639686	Not specified	UNKNOWN	TIVA vs TXA in Sinus Surgery to Evaluate Operative Blood Loss and Surgical Field Quality
NCT05693428	Not specified	COMPLETED	Influence of Anesthetics on Clinical Outcome During Cardiac Surgery in Adults
NCT05830864	Not specified	COMPLETED	Multicenter Retrospective Study of Isoflurane in Refractory and Super-Refractory Status Epilepticus
NCT06252207	Not specified	WITHDRAWN	Desflurane Versus Isoflurane for Speeding Postanesthetic Recovery and Hospital Discharge
NCT06307717	Not specified	COMPLETED	Effects of Volatile Anaesthetics on Incidence of Postoperative Depression and Anxiety in Elderly Patients
NCT06387836	Not specified	COMPLETED	LINC01844 as a Diagnostic Biomarker for POCD in Elderly Patients

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 desflurane, enflurane, halothane, iso	CPIC	CACNA1S;RYR1		yes

PharmGKB also curates 47 clinical and 33 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

58 molecules share ≥1 primary target. Top 58 by shared-target count:

Molecule	Source	Status	Shared targets
DICLOFENAC	ChEMBL + PubChem	Phase 4 (approved)	KCNK2, TRPA1
MEFENAMIC ACID	ChEMBL + PubChem	Phase 4 (approved)	KCNK2, TRPA1
MEXILETINE	ChEMBL + PubChem	Phase 4 (approved)	KCNK2, KCNK3
PROPAFENONE	ChEMBL + PubChem	Phase 4 (approved)	KCNK2, KCNK3
FLUFENAMIC ACID	ChEMBL	Phase 2	KCNK2, TRPA1
Caffeine	PubChem	Approved	KCNK2, TRPA1
Chloroform	PubChem	Approved	KCNK16, KCNK2
Lidocaine	PubChem	Approved	KCNK2, KCNK3
Quinine	PubChem	Approved	KCNK2, KCNK3
AMLODIPINE	ChEMBL + PubChem	Phase 4 (approved)	KCNK2
CARVEDILOL	ChEMBL + PubChem	Phase 4 (approved)	KCNK2
CHLORPROMAZINE	ChEMBL + PubChem	Phase 4 (approved)	KCNK2
DISULFIRAM	ChEMBL + PubChem	Phase 4 (approved)	TRPA1
FLUOXETINE	ChEMBL + PubChem	Phase 4 (approved)	KCNK2
FLUPHENAZINE	ChEMBL + PubChem	Phase 4 (approved)	KCNK2
HALOPERIDOL	ChEMBL + PubChem	Phase 4 (approved)	KCNK2
LOXAPINE	ChEMBL + PubChem	Phase 4 (approved)	KCNK2
NIFEDIPINE	ChEMBL + PubChem	Phase 4 (approved)	KCNK2
PIMOZIDE	ChEMBL + PubChem	Phase 4 (approved)	KCNK2
ROPIVACAINE	ChEMBL + PubChem	Phase 4 (approved)	KCNK3
BEPRIDIL	ChEMBL	Phase 4 (approved)	KCNK2
BUPIVACAINE	ChEMBL	Phase 4 (approved)	KCNK3
ETIDOCAINE	ChEMBL	Phase 4 (approved)	KCNK3
MENTHOL	ChEMBL	Phase 4 (approved)	TRPA1
NICOTINE	ChEMBL	Phase 4 (approved)	TRPA1
RESVERATROL	ChEMBL + PubChem	Phase 3 (approved)	TRPA1
CANNABINOL	ChEMBL	Phase 3	TRPA1
FLUPENTIXOL	ChEMBL	Phase 3	KCNK2
ICILLIN	ChEMBL	Phase 3	TRPA1
LEVOMENTHOL	ChEMBL	Phase 3	TRPA1
ALLICIN	ChEMBL	Phase 2	TRPA1
BAFREKALANT	ChEMBL	Phase 2	KCNK3
CANNABIDIVARIN	ChEMBL	Phase 2	TRPA1
CANNABIGEROL	ChEMBL	Phase 2	TRPA1
CARVACROL	ChEMBL	Phase 2	TRPA1
CHLORDANTOIN	ChEMBL	Phase 2	TRPA1
RG6341	ChEMBL	Phase 2	TRPA1
SALIRASIB	ChEMBL	Phase 2	TRPA1
SANGUINARIUM	ChEMBL	Phase 2	TRPA1
SIPATRIGINE	ChEMBL	Phase 2	KCNK2
TETRAHYDROCANNABIVARIN	ChEMBL	Phase 2	TRPA1
THYMOL	ChEMBL	Phase 2	TRPA1
Acetaldehyde	PubChem	Approved	TRPA1
camphor (synthetic)	PubChem	Approved	TRPA1
dalfampridine	PubChem	Approved	KCNK2
dronabinol	PubChem	Approved	TRPA1
ether	PubChem	Approved	KCNK3
Eugenol	PubChem	Approved	TRPA1
glyburide	PubChem	Approved	KCNK2
Haloperidol Decanoate	PubChem	Approved	KCNK2
Indomethacin	PubChem	Approved	KCNK2
menthol, unspecified form	PubChem	Approved	TRPA1
Mepivacaine	PubChem	Approved	KCNK3
Propylene Glycol	PubChem	Approved	TRPA1
Quinidine	PubChem	Approved	KCNK16
Riluzole	PubChem	Approved	KCNK2
Tetracaine	PubChem	Approved	KCNK3
theophylline	PubChem	Approved	KCNK2