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pentostatin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| enzyme inhibitors | 2098 | 53910-25-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 30 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 80 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.25 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 0.59 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.63 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.96 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 5.30 hours | Lombardo F, Berellini G, Obach RS |
| BA (Bioavailability) | 0 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,FLT3,GRK2,ITK,MAP2K6,MAP3K21,MAPK7,NTRK2,PDK1,PDK2,PDK4,PIK3CD,PRKDC,SIK2,TEK | 23 | |||
| kinase-selectivity-class | MAP2K6,PDK1 | 2 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 11, 1991 | FDA | HOSPIRA INC |
FDA Adverse Event Reporting System (Female)
None
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 |
|---|---|---|---|---|---|---|
| Renal tubular injury | 77.42 | 29.28 | 16 | 1112 | 1763 | 42618444 |
| Thrombotic microangiopathy | 67.25 | 29.28 | 22 | 1106 | 14760 | 42605447 |
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 |
|---|---|---|---|---|---|---|
| Renal tubular injury | 76.93 | 32.72 | 16 | 1707 | 3092 | 110584484 |
| Thrombotic microangiopathy | 56.27 | 32.72 | 20 | 1703 | 29129 | 110558447 |
| Neutropenia | 39.33 | 32.72 | 38 | 1685 | 374582 | 110212994 |
| Pancytopenia | 37.79 | 32.72 | 29 | 1694 | 209584 | 110377992 |
| Bronchopulmonary aspergillosis | 37.63 | 32.72 | 15 | 1708 | 29848 | 110557728 |
| Acute graft versus host disease | 33.28 | 32.72 | 11 | 1712 | 12870 | 110574706 |
| Graft versus host disease | 32.88 | 32.72 | 12 | 1711 | 18794 | 110568782 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01XX08 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Other antineoplastic agents |
| FDA MoA | N0000000233 | Nucleic Acid Synthesis Inhibitors |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D058892 | Adenosine Deaminase Inhibitors |
| FDA EPC | N0000175595 | Nucleoside Metabolic Inhibitor |
| CHEBI has role | CHEBI:35221 | antimetabolite |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:50445 | EC 3.5.4.4 (adenosine deaminase) inhibitor |
| CHEBI has role | CHEBI:75835 | anti-anaemic agent |
| CHEBI has role | CHEBI:76956 | <em>Aspergillus </em> metabolite |
| CHEBI has role | CHEBI:76969 | bacterial metabolite |
Related Drugs by ATC class:
L01XX Other antineoplastic agents 33 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hairy cell leukemia | indication | 118613001 | |
| Chronic lymphoid leukemia, disease | off-label use | 92814006 | |
| Pulmonary edema | contraindication | 19242006 | DOID:11396 |
| Infectious disease | contraindication | 40733004 | |
| Low blood pressure | contraindication | 45007003 | |
| Leukopenia | contraindication | 84828003 | DOID:615 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Liver function tests abnormal | contraindication | 166603001 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Pregnancy, function | contraindication | 289908002 | |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
| Bone marrow depression | contraindication | 307762000 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| CNS Toxicity | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.02 | acidic |
| pKa2 | 13.08 | acidic |
| pKa3 | 13.73 | acidic |
| pKa4 | 5.0 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Adenosine deaminase | Enzyme | INHIBITOR | IC50 | 10.80 | IUPHAR | CHEMBL | |||
| Adenosine deaminase | Enzyme | Ki | 11 | CHEMBL | |||||
| Adenosine deaminase | Enzyme | Ki | 10.42 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4020329 | VUID |
| N0000148177 | NUI |
| D00155 | KEGG_DRUG |
| 4020329 | VANDF |
| C0030896 | UMLSCUI |
| CHEBI:27834 | CHEBI |
| DCF | PDB_CHEM_ID |
| CHEMBL1580 | ChEMBL_ID |
| DB00552 | DRUGBANK_ID |
| D015649 | MESH_DESCRIPTOR_UI |
| 439693 | PUBCHEM_CID |
| 4805 | IUPHAR_LIGAND_ID |
| 4355 | INN_ID |
| 395575MZO7 | UNII |
| 8011 | RXNORM |
| 118563 | MMSL |
| 5256 | MMSL |
| d01356 | MMSL |
| 003617 | NDDF |
| 28149003 | SNOMEDCT_US |
| 387154004 | SNOMEDCT_US |
| 395575MZO7 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Nipent | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-0801 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 2 mg | INTRAVENOUS | NDA | 23 sections |