Stem definition | Drug id | CAS RN |
---|---|---|
enzyme inhibitors | 640 | 82009-34-5 |
Dose | Unit | Route |
---|---|---|
2 | g | P |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
S (Water solubility) | 25 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 70 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 59.78 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Vd (Volume of distribution) | 0.15 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 2.30 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.60 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 0.86 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Nov. 26, 1985 | FDA | MERCK |
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 |
---|---|---|---|---|---|---|
Seizure | 241.76 | 82.10 | 73 | 657 | 24393 | 2332962 |
Drug ineffective | 83.10 | 82.10 | 52 | 678 | 101572 | 2255783 |
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 |
---|---|---|---|---|---|---|
Seizure | 260.12 | 69.31 | 90 | 905 | 20351 | 1725435 |
Pathogen resistance | 186.80 | 69.31 | 38 | 957 | 1051 | 1744735 |
Drug ineffective | 158.72 | 69.31 | 89 | 906 | 63712 | 1682074 |
Sepsis | 110.73 | 69.31 | 48 | 947 | 19390 | 1726396 |
Septic shock | 99.51 | 69.31 | 35 | 960 | 8074 | 1737712 |
Multiple organ dysfunction syndrome | 98.76 | 69.31 | 36 | 959 | 9206 | 1736580 |
Toxic epidermal necrolysis | 88.26 | 69.31 | 24 | 971 | 2347 | 1743439 |
Drug resistance | 80.92 | 69.31 | 24 | 971 | 3206 | 1742580 |
Respiratory failure | 79.75 | 69.31 | 35 | 960 | 14470 | 1731316 |
Thrombocytopenia | 78.74 | 69.31 | 39 | 956 | 21210 | 1724576 |
Pyrexia | 76.33 | 69.31 | 50 | 945 | 46350 | 1699436 |
Toxic skin eruption | 69.77 | 69.31 | 19 | 976 | 1864 | 1743922 |
Source | Code | Description |
---|---|---|
ATC | J01DH51 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER BETA-LACTAM ANTIBACTERIALS Carbapenems |
FDA MoA | N0000175513 | Dipeptidase Inhibitors |
FDA EPC | N0000175514 | Renal Dehydropeptidase Inhibitor |
MeSH PA | D004791 | Enzyme Inhibitors |
MeSH PA | D011480 | Protease Inhibitors |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Bacterial septicemia | indication | 10001005 | DOID:0040085 |
Infection of skin AND/OR subcutaneous tissue | indication | 19824006 | |
Pneumonia due to Streptococcus | indication | 34020007 | |
Peritonitis | indication | 48661000 | |
Lower respiratory tract infection | indication | 50417007 | |
Pneumonia due to Escherichia coli | indication | 51530003 | |
Bacterial pneumonia | indication | 53084003 | DOID:874 |
Haemophilus influenzae pneumonia | indication | 70036007 | |
Abdominal abscess | indication | 75100008 | |
Endometritis | indication | 78623009 | DOID:1002 |
Infection of bone | indication | 111253001 | |
Female genital tract infection | indication | 125585007 | |
Infectious disease of abdomen | indication | 128070006 | |
Bacterial infection due to Klebsiella pneumoniae | indication | 186435004 | |
Bacterial endocarditis | indication | 301183007 | |
Bacterial urinary infection | indication | 312124009 | |
Infectious disorder of joint | indication | 363162000 | |
Acute exacerbation of chronic bronchitis | indication | 425748003 | |
Inflammatory Disease of Female Pelvic Organs | indication | ||
Enterobacter Pneumonia | indication | ||
Diabetic Foot Infection | indication | ||
Gram-Negative Aerobic Bacillary Pneumonia | indication | ||
Pyrexia of unknown origin | off-label use | 7520000 | |
Inhalational anthrax | off-label use | 11389007 | |
Cutaneous anthrax | off-label use | 84980006 | DOID:7426 |
Gastrointestinal anthrax | off-label use | 111798006 | DOID:13386 |
Infection by Campylobacter fetus | off-label use | 111835002 | |
Gas gangrene caused by clostridium perfringens | off-label use | 266093005 | |
Anthrax | off-label use | 409498004 | DOID:7427 |
Melioidosis | off-label use | 428111003 | DOID:5052 |
Clostridium Perfringens Empyema | off-label use | ||
Pseudomonas Respiratory Tract Infection in Cystic Fibrosis | off-label use | ||
Kidney disease | contraindication | 90708001 | DOID:557 |
Seizure disorder | contraindication | 128613002 | |
Lesion of brain | contraindication | 301766008 | |
Pseudomembranous enterocolitis | contraindication | 397683000 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 2.08 | acidic |
pKa2 | 3.82 | acidic |
pKa3 | 12.31 | acidic |
pKa4 | 9.35 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
EQ 500MG BASE/VIAL | RECARBRIO | MSD MERCK CO | N212819 | July 16, 2019 | RX | POWDER | INTRAVENOUS | 8487093 | Nov. 19, 2029 | TREATMENT OF COMPLICATED INTRA-ABDOMINAL INFECTIONS (CIAI) |
EQ 500MG BASE/VIAL | RECARBRIO | MSD MERCK CO | N212819 | July 16, 2019 | RX | POWDER | INTRAVENOUS | 8487093 | Nov. 19, 2029 | TREATMENT OF COMPLICATED URINARY TRACT INFECTIONS, INCLUDING PYELONEPHRITIS (CUTI) |
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Dipeptidase 1 | Enzyme | INHIBITOR | Ki | 6.96 | WOMBAT-PK | CHEMBL | |||
Dipeptidase 1 | Enzyme | Ki | 6.96 | CHEMBL |
ID | Source |
---|---|
4019679 | VUID |
N0000147771 | NUI |
C0008777 | UMLSCUI |
D02194 | KEGG_DRUG |
141A6AMN38 | UNII |
5457 | INN_ID |
81129-83-1 | SECONDARY_CAS_RN |
422591002 | SNOMEDCT_US |
2540 | RXNORM |
96058005 | SNOMEDCT_US |
d04402 | MMSL |
4019679 | VANDF |
004539 | NDDF |
CHEMBL766 | ChEMBL_ID |
CIL | PDB_CHEM_ID |
DB01597 | DRUGBANK_ID |
CHEBI:3697 | CHEBI |
5166 | IUPHAR_LIGAND_ID |
CHEMBL1201057 | ChEMBL_ID |
D015377 | MESH_DESCRIPTOR_UI |
6435415 | PUBCHEM_CID |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
PRIMAXIN | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0006-3514 | INJECTION, POWDER, FOR SOLUTION | 250 mg | INTRAVENOUS | NDA | 16 sections |
PRIMAXIN | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0006-3516 | INJECTION, POWDER, FOR SOLUTION | 500 mg | INTRAVENOUS | NDA | 16 sections |
PRIMAXIN | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0006-3551 | INJECTION, POWDER, FOR SOLUTION | 250 mg | INTRAVENOUS | ANDA | 16 sections |
PRIMAXIN | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0006-3552 | INJECTION, POWDER, FOR SOLUTION | 500 mg | INTRAVENOUS | ANDA | 16 sections |
RECARBRIO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-3856 | INJECTION, POWDER, FOR SOLUTION | 500 mg | INTRAVENOUS | NDA | 17 sections |
Imipenem and Cilastatin | HUMAN PRESCRIPTION DRUG LABEL | 2 | 63323-322 | INJECTION, POWDER, FOR SOLUTION | 500 mg | INTRAVENOUS | ANDA | 16 sections |
Imipenem and Cilastatin | HUMAN PRESCRIPTION DRUG LABEL | 2 | 63323-349 | INJECTION, POWDER, FOR SOLUTION | 250 mg | INTRAVENOUS | ANDA | 16 sections |