Insulin Human
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Also known as ActrapidAfrezzaBiosulin rCapsulinExuberaExubera (inhaled insulin human)High molecular weight insulin humanHuman insulinHumulinHumulin brHumulin rInpremziaIns humulin rInsulinInsulin (human)Insulin human (biosynthesis)Insulin human (rdna)Insulin human (synthesis)Insulin human lente
Summary
Insulin Human (CHEMBL1201631) is an approved protein (ATC A10AF01) targeting INSR; indicated across 54 conditions including diabetes mellitus and type 2 diabetes mellitus.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Protein
- ATC class: A10AF01 (+4 more)
- Targets: 1 (INSR)
- Indications: 54 conditions
- Clinical trials: 612
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1201631 |
| Name | Insulin Human |
| Type | Protein |
| Max phase | 4 |
| ATC | A10AF01, A10AC01, A10AD01, A10AB01, A10AE01 |
Also known as: Actrapid, Afrezza, Biosulin r, Capsulin, Exubera, Exubera (inhaled insulin human), High molecular weight insulin human, Human insulin, Humulin, Humulin br, Humulin r, Inpremzia
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 |
|---|---|---|---|---|---|
| INSR | Insulin receptor | Agonist | 0.8% | P06213 |
Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Tyrosine-protein kinase Lck, Insulin receptor.
Bioactivity
ChEMBL activities: 2 potent at pChembl ≥ 5 of 3 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| P15127 | 8.74 | Ki | 1.82 | nM | CHEMBL_ACT_7773832 |
| P15127 | 8.71 | IC50 | 1.93 | nM | CHEMBL_ACT_7773831 |
Target pathways
Aggregated over 1 target gene(s): INSR.
Top Reactome pathways
11 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| PIP3 activates AKT signaling | 1 | INSR |
| Signal Transduction | 1 | INSR |
| Negative regulation of the PI3K/AKT network | 1 | INSR |
| PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling | 1 | INSR |
| IRS activation | 1 | INSR |
| Signal attenuation | 1 | INSR |
| Insulin receptor signalling cascade | 1 | INSR |
| Signaling by Insulin receptor | 1 | INSR |
| Insulin receptor recycling | 1 | INSR |
| Intracellular signaling by second messengers | 1 | INSR |
| Signaling by Receptor Tyrosine Kinases | 1 | INSR |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| positive regulation of receptor internalization | 1 |
| heart morphogenesis | 1 |
| regulation of DNA-templated transcription | 1 |
| receptor-mediated endocytosis | 1 |
| G protein-coupled receptor signaling pathway | 1 |
| learning | 1 |
| memory | 1 |
| positive regulation of cell population proliferation | 1 |
| insulin receptor signaling pathway | 1 |
| epidermis development | 1 |
| male gonad development | 1 |
| male sex determination | 1 |
| adrenal gland development | 1 |
| positive regulation of cell migration | 1 |
| exocrine pancreas development | 1 |
Indications & clinical
Indications
54 indications (2 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 |
|---|---|---|---|
| diabetes mellitus | 4 | MONDO:0005015 | EFO:0000400 |
| type 2 diabetes mellitus | 4 | MONDO:0005148 | MONDO:0005148 |
| hyperglycemia | 3 | MONDO:0002909 | HP:0003074 |
| myocardial infarction | 3 | MONDO:0005068 | EFO:0000612 |
| gestational diabetes | 3 | MONDO:0005406 | EFO:0004593 |
| congestive heart failure | 3 | MONDO:0005009 | EFO:0000373 |
| acute coronary syndrome | 3 | MONDO:0005542 | EFO:0005672 |
| toxic shock syndrome | 3 | MONDO:0001881 | EFO:0006834 |
| intermediate coronary syndrome | 3 | MONDO:0006805 | EFO:1000985 |
| hypertensive disorder | 3 | MONDO:0005044 | EFO:0000537 |
| atherosclerosis | 3 | MONDO:0005311 | EFO:0003914 |
| major depressive disorder | 3 | MONDO:0002009 | MONDO:0002009 |
| hypogonadism | 3 | MONDO:0002146 | MONDO:0002146 |
| coronary artery disorder | 3 | MONDO:0005010 | EFO:0001645 |
| acute myocardial infarction | 3 | MONDO:0004781 | EFO:0008583 |
| type 1 diabetes mellitus | 3 | MONDO:0005147 | MONDO:0005147 |
| bipolar disorder | 3 | MONDO:0004985 | MONDO:0004985 |
| nicotine dependence | 2 | MONDO:0008575 | EFO:0003768 |
| metabolic dysfunction-associated steatotic liver disease | 2 | MONDO:0013209 | EFO:0003095 |
| hypoglycemia | 2 | MONDO:0004946 | HP:0001943 |
| diabetic neuropathy | 2 | MONDO:0006626 | EFO:1000783 |
| acute kidney injury | 2 | MONDO:0002492 | HP:0001919 |
| persian gulf syndrome | 2 | MONDO:0005907 | EFO:0007430 |
| stroke disorder | 2 | MONDO:0005098 | EFO:0000712 |
| post-traumatic stress disorder | 2 | MONDO:0005146 | EFO:0001358 |
| burn | 2 | MONDO:0043519 | EFO:0009516 |
| multiple system atrophy | 2 | MONDO:0007803 | EFO:1001050 |
| Parkinson disease | 2 | MONDO:0005180 | MONDO:0005180 |
| hyperlipidemia | 2 | MONDO:0021187 | MONDO:0021187 |
| diabetic kidney disease | 2 | MONDO:0005016 | EFO:0000401 |
| frontotemporal dementia | 2 | MONDO:0017276 | MONDO:0017276 |
| obesity disorder | 1 | MONDO:0011122 | EFO:0001073 |
| chronic progressive multiple sclerosis | 1 | MONDO:0005284 | EFO:0003840 |
| relapsing-remitting multiple sclerosis | 1 | MONDO:0005314 | EFO:0003929 |
| hyperinsulinism | 1 | MONDO:0002177 | HP:0000842 |
| delirium | 1 | MONDO:0045057 | EFO:0009267 |
| dry eye syndrome | 1 | MONDO:0006733 | EFO:1000906 |
| injury | 1 | MONDO:0021178 | EFO:0000546 |
| cardiac arrest | 1 | MONDO:0000745 | EFO:0009492 |
| severe acute respiratory syndrome | 1 | MONDO:0005091 | MONDO:0100096 |
| glaucoma | 1 | MONDO:0005041 | MONDO:0005041 |
| keloid | 1 | MONDO:0005348 | EFO:0004212 |
| alcohol abuse | 1 | MONDO:0002046 | MONDO:0007079 |
| carpal tunnel syndrome | 0 | MONDO:0007275 | EFO:0004143 |
10 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 612.
Phase distribution
| Phase | Trials |
|---|---|
| Not specified | 193 |
| PHASE4 | 140 |
| PHASE3 | 88 |
| PHASE2 | 77 |
| PHASE1 | 59 |
| EARLY_PHASE1 | 22 |
| PHASE1/PHASE2 | 17 |
| PHASE2/PHASE3 | 16 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT03463564 | PHASE4 | RECRUITING | Insulin Pump vs Multiple Daily Injections of Insulin and Glyco-metabolic Control in Type 1 Diabetic Patients |
| NCT03527537 | PHASE4 | ACTIVE_NOT_RECRUITING | Gestational Diabetes and Pharmacotherapy (GAP) |
| NCT04416269 | PHASE4 | ACTIVE_NOT_RECRUITING | Oral Anti Diabetic Agents in the Hospital |
| NCT06017362 | PHASE4 | RECRUITING | Clinical Trial to Determine the Efficacy and Safety of Insulin Eye Drops in Dry Eye in Patients with Topical Hypotensors |
| NCT06408532 | PHASE4 | NOT_YET_RECRUITING | The Efficacy and Safety of Insulin Degludec/Liraglutide Combination (IDegLira) in Patients With Type 2 Diabetes |
| NCT06445946 | PHASE4 | RECRUITING | DECIDE: A Comparative Effectiveness Trial of Metformin Versus Insulin for the Treatment of Gestational Diabetes |
| NCT06699810 | PHASE4 | ACTIVE_NOT_RECRUITING | Modeling Ketosis-Prone Diabetes Remission Via Diverse Mechanisms of Glucotoxicity |
| NCT06781775 | PHASE4 | RECRUITING | GDM: Insulin with or Without Metformin? |
| NCT06925334 | PHASE4 | ENROLLING_BY_INVITATION | A Study Comparing Degu Insulin Liraglutide Injection With Premixed Insulin on the Prognosis of Diabetes Mellitus |
| NCT06939959 | PHASE4 | RECRUITING | Evaluating the Efficacy of Topical Insulin for the Restoration of Ocular Surface Interface in Dry Eye Disease. |
| NCT07293715 | PHASE4 | RECRUITING | Permissive Versus Strict Intrapartum Glucose Management in Type 1 Diabetes (PRISM-T1D) |
| NCT07494084 | PHASE4 | NOT_YET_RECRUITING | Sleep Loss and Circadian Misalignment - Mechanisms of Insulin Resistance |
| NCT00118963 | PHASE4 | COMPLETED | Effect of Repaglinide Versus Metformin Treatment in Non-Obese Patients With Type-2-Diabetes |
| NCT00160485 | PHASE4 | WITHDRAWN | Glyburide Compared to Insulin in the Management of White’s Classification A2 Gestational Diabetes |
| NCT00191282 | PHASE4 | COMPLETED | Hyperglycemia and Cardiovascular Outcomes With Type 2 Diabetes |
| NCT00276393 | PHASE4 | COMPLETED | Treatment Trial Evaluating Long Acting Insulin in Type 1 Diabetes |
| NCT00309465 | PHASE4 | COMPLETED | Perioperative Insulin Glargine Dosing Study |
| NCT00315952 | PHASE4 | COMPLETED | Study to Estimate the Effects of Inhaled Versus Intravenous (IV) Infusion of Human Insulin in Subjects With Type 1 Diabetes |
| NCT00340613 | PHASE4 | COMPLETED | Lunch Time Insulin Injection by School Nurse for Poorly Controlled Diabetes |
| NCT00346996 | PHASE4 | COMPLETED | Insulin Analogues and Severe Hypoglycaemia |
| NCT00353834 | PHASE4 | COMPLETED | The Effect of Exenatide Compared to Lantus Insulin on Vascular Function in Type 2 Diabetes |
| NCT00362778 | PHASE4 | COMPLETED | Intensive Insulin Therapy in Non-diabetic Patients With Acute Myocardial Infarction and Hyperglycaemia |
| NCT00365170 | PHASE4 | COMPLETED | Efficacy and Safety of Insulin Aspart vs. Human Insulin During Pregnancy by Women With Type 1 Diabetes |
| NCT00384085 | PHASE4 | COMPLETED | Insulin Glargine All to Target Trial |
| NCT00420095 | PHASE4 | COMPLETED | A Study for Patients With Diabetes Mellitus (IOPA) |
| NCT00442767 | PHASE4 | COMPLETED | Post-meal Insulin Dosing With Adjuvant Pre-meal Pramlintide in Children With Type 1 Diabetes Mellitus |
| NCT00505505 | PHASE4 | UNKNOWN | Intensive Insulin Therapy for Strict Glycemic Control in Neurosurgical Patients: Safety and Efficacy |
| NCT00513201 | PHASE4 | COMPLETED | Lyspro Insulin vs Regular Insulin in Cirrhotic Patients |
| NCT00523393 | PHASE4 | UNKNOWN | Prospective Influence of Bedtime Insulin Glargine on Mobilization and Function of Endothelial Progenitor Cells |
| NCT00535925 | PHASE4 | COMPLETED | Nephropathy In Type 2 Diabetes and Cardio-renal Events |
| NCT00596687 | PHASE4 | COMPLETED | Basal Bolus Insulin Versus SSRI in Type 2 Diabetes Undergoing General Surgery |
| NCT00646581 | PHASE4 | COMPLETED | Effect of Single Dose Intranasal Insulin On Cognitive Function |
| NCT00663624 | PHASE4 | WITHDRAWN | Management of Hyperglycemia in the ER: A Randomized Clinical Trial of a Subcutaneous Insulin Aspart Protocol Coupled With Rapid Initiation of Basal Bolus Insulin Prior to Hospital Admission Versus Usual Care |
| NCT00676819 | PHASE4 | COMPLETED | Comparison of the Pharmacodynamics and Pharmacokinetics of Insulin Aspart and Human Insulin in Elderly People With Type 2 Diabetes |
| NCT00770445 | PHASE4 | COMPLETED | Efficacy of Pioglitazone and Metformin on Cardiovascular Risk in Subjects With Insulin-Treated Type 2 Diabetes Mellitus. |
| NCT00779701 | PHASE4 | COMPLETED | Strict Glycemic Control by Insulin Infusion:Observations on Emergency Department Initiation |
| NCT00780026 | PHASE4 | COMPLETED | Intraoperative Glucose Control in Liver Transplant |
| NCT00841919 | PHASE4 | COMPLETED | Insulin Therapy in the Hospital Comparing Two Protocols |
| NCT00863629 | PHASE4 | COMPLETED | Tight Glycemic Control Increases Cardiac Stem Cells During Acute Myocardial Infarction |
| NCT00941148 | PHASE4 | COMPLETED | Beta-Cell Function of Insulin Glargine Compared to Neutral Protamine Hagedorn (NPH) Insuline and to Insulin Detemir in Combination With Metformin |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
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.
37 molecules share ≥1 primary target. Top 37 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | INSR |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | INSR |
| CERITINIB | ChEMBL | Phase 4 (approved) | INSR |
| ENTRECTINIB | ChEMBL | Phase 4 (approved) | INSR |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | INSR |
| INFIGRATINIB | ChEMBL | Phase 4 (approved) | INSR |
| LAPATINIB | ChEMBL | Phase 4 (approved) | INSR |
| NERATINIB | ChEMBL | Phase 4 (approved) | INSR |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | INSR |
| OSIMERTINIB | ChEMBL | Phase 4 (approved) | INSR |
| SORAFENIB | ChEMBL | Phase 4 (approved) | INSR |
| SUNITINIB | ChEMBL | Phase 4 (approved) | INSR |
| DOVITINIB | ChEMBL | Phase 3 | INSR |
| LESTAURTINIB | ChEMBL | Phase 3 | INSR |
| LINIFANIB | ChEMBL | Phase 3 | INSR |
| LINSITINIB | ChEMBL | Phase 3 | INSR |
| BMS-754807 | ChEMBL | Phase 2 | INSR |
| CENISERTIB | ChEMBL | Phase 2 | INSR |
| ELLAGIC ACID | ChEMBL | Phase 2 | INSR |
| FORETINIB | ChEMBL | Phase 2 | INSR |
| ILORASERTIB | ChEMBL | Phase 2 | INSR |
| OSI-632 | ChEMBL | Phase 2 | INSR |
| R-406 | ChEMBL | Phase 2 | INSR |
| SU-014813 | ChEMBL | Phase 2 | INSR |
| TOZASERTIB | ChEMBL | Phase 2 | INSR |
| Afatinib | PubChem | Approved | INSR |
| belumosudil | PubChem | Approved | INSR |
| Belzutifan | PubChem | Approved | INSR |
| Binimetinib | PubChem | Approved | INSR |
| dacomitinib | PubChem | Approved | INSR |
| Fostamatinib | PubChem | Approved | INSR |
| Gefitinib | PubChem | Approved | INSR |
| Idelalisib | PubChem | Approved | INSR |
| Pazopanib | PubChem | Approved | INSR |
| regorafenib | PubChem | Approved | INSR |
| Selumetinib | PubChem | Approved | INSR |
| Trametinib | PubChem | Approved | INSR |
Related Atlas pages
- Genes: INSR
- Diseases: diabetes mellitus, type 2 diabetes mellitus, hyperglycemia, myocardial infarction, gestational diabetes, congestive heart failure, acute coronary syndrome, toxic shock syndrome, intermediate coronary syndrome, hypertensive disorder, atherosclerosis, major depressive disorder, hypogonadism, coronary artery disorder, acute myocardial infarction, type 1 diabetes mellitus, bipolar disorder
- Drugs: Crizotinib, Brigatinib, Ceritinib, Entrectinib, Fedratinib, Infigratinib, Lapatinib, Neratinib, Nintedanib, Osimertinib, Sorafenib, Sunitinib, Dovitinib, Lestaurtinib, Linifanib, Linsitinib, Afatinib, belumosudil, Belzutifan, Binimetinib, dacomitinib, Fostamatinib, Gefitinib, Idelalisib, Pazopanib, regorafenib, Selumetinib, Trametinib