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amifostine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| insecticides, anthelminthics, pesticides etc., phosphorous derivatives | 156 | 20537-88-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1.70 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.69 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 105 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 99 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.09 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 30.65 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 0.15 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 18.70 mg/mL | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHUK,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,FGFR1,FLT1,FLT3,GRK2,GSK3B,IGF1R,IKBKB,ITK,JAK1,JAK2,JAK3,KDR,MAP2K6,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK10,MAPK7,MAPK9,MAPKAPK2,MARK4,MTOR,NTRK1,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIK3CD,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,SRC,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ULK2,ZAP70 | 70 | |||
| kinase-selectivity-class | ACVRL1,ALK,AURKB,AXL,BRAF,CAMK2D,CDK1,CDK4,CDK6,CDK7,CDK9,CHEK1,CHUK,DDR1,DYRK1B,EPHB4,ERBB2,FLT3,GRK2,IRAK1,IRAK3,IRAK4,MAP2K6,MAP3K21,MAP3K7,MAP4K1,MAPK7,PAK4,PIK3CB,PIK3CD,PRKCD,SIK2,SIK3,STK33,SYK,TEK,ULK2,ZAP70 | 38 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 8, 1995 | FDA | CLINIGEN HLTHCARE |
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 |
|---|---|---|---|---|---|---|
| Pyrexia | 44.50 | 42.45 | 40 | 740 | 660445 | 89967222 |
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 |
|---|---|---|---|---|---|---|
| Mucosal inflammation | 146.75 | 36.28 | 61 | 1777 | 49313 | 42570184 |
| Laryngeal pain | 132.21 | 36.28 | 29 | 1809 | 2593 | 42616904 |
| Pyrexia | 90.74 | 36.28 | 97 | 1741 | 393945 | 42225552 |
| Chills | 67.80 | 36.28 | 45 | 1793 | 94021 | 42525476 |
| Hypotension | 65.36 | 36.28 | 67 | 1771 | 257564 | 42361933 |
| Soft tissue disorder | 63.35 | 36.28 | 13 | 1825 | 841 | 42618656 |
| Dehydration | 55.44 | 36.28 | 47 | 1791 | 141720 | 42477777 |
| Rash | 51.08 | 36.28 | 61 | 1777 | 276893 | 42342604 |
| Nausea | 50.88 | 36.28 | 73 | 1765 | 396726 | 42222771 |
| Dermatitis | 50.27 | 36.28 | 19 | 1819 | 11856 | 42607641 |
| Vomiting | 44.11 | 36.28 | 58 | 1780 | 289665 | 42329832 |
| Injection site reaction | 41.78 | 36.28 | 18 | 1820 | 15703 | 42603794 |
| Radiation skin injury | 41.30 | 36.28 | 9 | 1829 | 776 | 42618721 |
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 |
|---|---|---|---|---|---|---|
| Laryngeal pain | 166.02 | 33.52 | 36 | 2426 | 5939 | 110580898 |
| Mucosal inflammation | 119.76 | 33.52 | 53 | 2409 | 96088 | 110490749 |
| Pyrexia | 113.45 | 33.52 | 118 | 2344 | 898147 | 109688690 |
| Hypotension | 88.64 | 33.52 | 81 | 2381 | 523768 | 110063069 |
| Chills | 83.02 | 33.52 | 52 | 2410 | 190528 | 110396309 |
| Dehydration | 71.56 | 33.52 | 55 | 2407 | 279456 | 110307381 |
| Nausea | 68.56 | 33.52 | 108 | 2354 | 1235582 | 109351255 |
| Soft tissue disorder | 63.92 | 33.52 | 15 | 2447 | 3509 | 110583328 |
| Radiation skin injury | 63.51 | 33.52 | 13 | 2449 | 1619 | 110585218 |
| Dermatitis | 60.84 | 33.52 | 23 | 2439 | 27814 | 110559023 |
| Injection site erythema | 60.25 | 33.52 | 33 | 2429 | 94143 | 110492694 |
| Vomiting | 55.08 | 33.52 | 83 | 2379 | 910592 | 109676245 |
| Rash | 54.20 | 33.52 | 78 | 2384 | 820886 | 109765951 |
| Rash papular | 53.83 | 33.52 | 21 | 2441 | 27618 | 110559219 |
| Injection site reaction | 45.62 | 33.52 | 27 | 2435 | 89043 | 110497794 |
| Injection site rash | 39.35 | 33.52 | 16 | 2446 | 23403 | 110563434 |
| Pharyngitis | 38.28 | 33.52 | 16 | 2446 | 25082 | 110561755 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | V03AF05 | VARIOUS ALL OTHER THERAPEUTIC PRODUCTS ALL OTHER THERAPEUTIC PRODUCTS Detoxifying agents for antineoplastic treatment |
| CHEBI has role | CHEBI:22586 | antioxidant |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:50266 | prodrug |
| CHEBI has role | CHEBI:66987 | radiation protective agent |
| CHEBI has role | CHEBI:75835 | anti-anaemic agent |
| MeSH PA | D011837 | Radiation-Protective Agents |
| MeSH PA | D020011 | Protective Agents |
Related Drugs by ATC class:
V03AF Detoxifying agents for antineoplastic treatment 10 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Prevention of Xerostomia Secondary to Radiation Therapy | indication | ||
| Prevention of Cancer Chemotherapy-Induced Renal Impairment | indication | ||
| Myelodysplastic syndrome | off-label use | 109995007 | |
| Drug-induced mucositis | off-label use | 403666006 | |
| Chemotherapy-induced neutropenia | off-label use | 425229001 | |
| Prevention of Chemotherapy-Induced Neurotoxicity | off-label use | ||
| Prevention of Radiation Therapy-Induced Mucositis | off-label use | ||
| Hypocalcemia | contraindication | 5291005 | |
| Hypovolemia | contraindication | 28560003 | |
| Dehydration | contraindication | 34095006 | |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Low blood pressure | contraindication | 45007003 | |
| Chronic heart failure | contraindication | 48447003 | |
| Cerebrovascular accident | contraindication | 230690007 | |
| Transient ischemic attack | contraindication | 266257000 | DOID:224 |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Myocardial ischemia | contraindication | 414795007 | DOID:3393 |
| Vomiting | contraindication | 422400008 | |
| Nausea | contraindication | 422587007 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.67 | acidic |
| pKa2 | 10.06 | Basic |
| pKa3 | 8.46 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| D(3) dopamine receptor | GPCR | Ki | 6.18 | DRUG MATRIX | |||||
| Alkaline phosphatase, tissue-nonspecific isozyme | Enzyme | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4020970 | VUID |
| N0000148443 | NUI |
| D00226 | KEGG_DRUG |
| 1545987 | RXNORM |
| C0015020 | UMLSCUI |
| CHEBI:2636 | CHEBI |
| CHEMBL1006 | ChEMBL_ID |
| DB01143 | DRUGBANK_ID |
| D004999 | MESH_DESCRIPTOR_UI |
| 2141 | PUBCHEM_CID |
| M487QF2F4V | UNII |
| 133029 | MMSL |
| 4164 | MMSL |
| d03868 | MMSL |
| 112901-68-5 | SECONDARY_CAS_RN |
| 4020970 | VANDF |
| 005536 | NDDF |
| 108823002 | SNOMEDCT_US |
| 386923005 | SNOMEDCT_US |
| M487QF2F4V | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Ethyol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 83107-030 | INJECTION | 500 mg | INTRAVENOUS | NDA | 26 sections |