Stem definition | Drug id | CAS RN |
---|---|---|
enzyme inhibitors | 640 | 82009-34-5 |
Dose | Unit | Route |
---|---|---|
2 | g | P |
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 ยตM/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 | |
June 23, 2021 | PMDA | MSD K.K. |
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 | 142.68 | 28.72 | 71 | 1546 | 117803 | 50485704 |
Multiple organ dysfunction syndrome | 50.97 | 28.72 | 27 | 1590 | 50310 | 50553197 |
Septic shock | 37.22 | 28.72 | 23 | 1594 | 57152 | 50546355 |
Generalised tonic-clonic seizure | 35.04 | 28.72 | 17 | 1600 | 26293 | 50577214 |
Renal failure | 32.47 | 28.72 | 27 | 1590 | 106606 | 50496901 |
Heparin-induced thrombocytopenia | 29.52 | 28.72 | 9 | 1608 | 3956 | 50599551 |
Rash maculo-papular | 28.95 | 28.72 | 15 | 1602 | 26626 | 50576881 |
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 | 124.66 | 24.88 | 83 | 2317 | 93040 | 29479087 |
Septic shock | 56.41 | 24.88 | 44 | 2356 | 62516 | 29509611 |
Multiple organ dysfunction syndrome | 49.67 | 24.88 | 41 | 2359 | 63075 | 29509052 |
Eosinophilia | 32.49 | 24.88 | 21 | 2379 | 22140 | 29549987 |
Toxic epidermal necrolysis | 31.12 | 24.88 | 19 | 2381 | 18134 | 29553993 |
Hepatic cytolysis | 26.12 | 24.88 | 13 | 2387 | 8334 | 29563793 |
Pseudomonas infection | 25.64 | 24.88 | 14 | 2386 | 10838 | 29561289 |
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 | 188.22 | 26.49 | 118 | 3627 | 166774 | 64328213 |
Multiple organ dysfunction syndrome | 92.65 | 26.49 | 63 | 3682 | 101350 | 64393637 |
Septic shock | 76.65 | 26.49 | 57 | 3688 | 105380 | 64389607 |
Generalised tonic-clonic seizure | 49.28 | 26.49 | 30 | 3715 | 39827 | 64455160 |
Eosinophilia | 42.86 | 26.49 | 27 | 3718 | 38049 | 64456938 |
Renal failure | 41.73 | 26.49 | 52 | 3693 | 181636 | 64313351 |
Toxic epidermal necrolysis | 40.95 | 26.49 | 26 | 3719 | 37140 | 64457847 |
Agranulocytosis | 40.27 | 26.49 | 26 | 3719 | 38203 | 64456784 |
Thrombocytopenia | 34.72 | 26.49 | 53 | 3692 | 223748 | 64271239 |
Pseudomonas infection | 34.43 | 26.49 | 18 | 3727 | 17865 | 64477122 |
Dermatitis exfoliative | 33.89 | 26.49 | 15 | 3730 | 10337 | 64484650 |
Stevens-Johnson syndrome | 32.92 | 26.49 | 22 | 3723 | 34227 | 64460760 |
Sepsis | 32.19 | 26.49 | 52 | 3693 | 230289 | 64264698 |
Drug reaction with eosinophilia and systemic symptoms | 32.11 | 26.49 | 26 | 3719 | 54191 | 64440796 |
Pathogen resistance | 31.13 | 26.49 | 15 | 3730 | 12528 | 64482459 |
Epilepsy | 30.94 | 26.49 | 21 | 3724 | 33510 | 64461477 |
Gamma-glutamyltransferase increased | 30.30 | 26.49 | 24 | 3721 | 48486 | 64446501 |
Haemodialysis | 29.52 | 26.49 | 16 | 3729 | 17061 | 64477926 |
Respiratory failure | 29.06 | 26.49 | 41 | 3704 | 161142 | 64333845 |
Disseminated intravascular coagulation | 26.89 | 26.49 | 19 | 3726 | 32329 | 64462658 |
Hepatic cytolysis | 26.64 | 26.49 | 14 | 3731 | 14035 | 64480952 |
None
Source | Code | Description |
---|---|---|
ATC | J01DH51 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER BETA-LACTAM ANTIBACTERIALS Carbapenems |
ATC | J01DH56 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER BETA-LACTAM ANTIBACTERIALS Carbapenems |
FDA MoA | N0000175513 | Dipeptidase Inhibitors |
FDA EPC | N0000175514 | Renal Dehydropeptidase Inhibitor |
CHEBI has role | CHEBI:35703 | Xenobiotic |
CHEBI has role | CHEBI:37670 | protease inhibitors |
CHEBI has role | CHEBI:76926 | dipeptide hydrolase inhibitors |
CHEBI has role | CHEBI:78298 | environmental contaminants |
MeSH PA | D004791 | Enzyme Inhibitors |
MeSH PA | D011480 | Protease Inhibitors |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Bacterial septicemia | indication | 10001005 | DOID:0040085 |
Infection caused by Pseudomonas aeruginosa strain resistant to carbapenem antimicrobial drugs | indication | 11218009 | |
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 | |
Infection caused by Escherichia coli strain resistant to carbapenem antimicrobial drugs | indication | 71057007 | |
Infection caused by Serratia spp resistant to carbapenem antimicrobial drugs | indication | 71120004 | |
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 | |
Infection caused by Enterococcus spp resistant to carbapenem antimicrobial drugs | indication | 406574007 | |
Acute exacerbation of chronic bronchitis | indication | 425748003 | |
Infection caused by Klebsiella spp resistant to carbapenem antimicrobial drugs | indication | 721756002 | |
Infection caused by Acinetobacter spp resistant to carbapenem antimicrobial drugs | indication | 840588006 | |
Infection caused by Citrobacter spp resistant to carbapenem antimicrobial drugs | indication | 1137353009 | |
Enterobacter Pneumonia | indication | ||
Inflammatory Disease of Female Pelvic Organs | 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 |
None
None
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;500MG/VIAL;250MG/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;500MG/VIAL;250MG/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) |
EQ 500MG BASE/VIAL;500MG/VIAL;250MG/VIAL | RECARBRIO | MSD MERCK CO | N212819 | July 16, 2019 | RX | POWDER | INTRAVENOUS | 8487093 | Nov. 19, 2029 | TREATMENT OF HOSPITAL-ACQUIRED BACTERIAL PNEUMONIA AND VENTILATOR-ASSOCIATED BACTERIAL PNEUMONIA (HABP/VABP) |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
EQ 500MG BASE/VIAL;500MG/VIAL;250MG/VIAL | RECARBRIO | MSD MERCK CO | N212819 | July 16, 2019 | RX | POWDER | INTRAVENOUS | July 16, 2024 | NEW CHEMICAL ENTITY |
EQ 500MG BASE/VIAL;500MG/VIAL;250MG/VIAL | RECARBRIO | MSD MERCK CO | N212819 | July 16, 2019 | RX | POWDER | INTRAVENOUS | July 16, 2029 | GENERATING ANTIBIOTIC INCENTIVES NOW |
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 |
D02194 | KEGG_DRUG |
81129-83-1 | SECONDARY_CAS_RN |
2540 | RXNORM |
4017968 | VANDF |
4019679 | VANDF |
C0008777 | UMLSCUI |
CHEBI:3697 | CHEBI |
CIL | PDB_CHEM_ID |
CHEMBL766 | ChEMBL_ID |
DB01597 | DRUGBANK_ID |
CHEMBL1201057 | ChEMBL_ID |
D015377 | MESH_DESCRIPTOR_UI |
6435415 | PUBCHEM_CID |
5166 | IUPHAR_LIGAND_ID |
5457 | INN_ID |
141A6AMN38 | UNII |
32313 | MMSL |
4447 | MMSL |
d04402 | MMSL |
001086 | NDDF |
004539 | NDDF |
422591002 | SNOMEDCT_US |
734464004 | SNOMEDCT_US |
96058005 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
PRIMAXINIV | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0006-3514 | INJECTION, POWDER, FOR SOLUTION | 250 mg | INTRAVENOUS | NDA | 25 sections |
PRIMAXINIV | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0006-3516 | INJECTION, POWDER, FOR SOLUTION | 500 mg | INTRAVENOUS | NDA | 25 sections |
PRIMAXINIV | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0006-3551 | INJECTION, POWDER, FOR SOLUTION | 250 mg | INTRAVENOUS | ANDA | 25 sections |
PRIMAXINIV | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0006-3552 | INJECTION, POWDER, FOR SOLUTION | 500 mg | INTRAVENOUS | ANDA | 25 sections |
RECARBRIO | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0006-3856 | INJECTION, POWDER, FOR SOLUTION | 500 mg | INTRAVENOUS | NDA | 29 sections |
RECARBRIO | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0006-3856 | INJECTION, POWDER, FOR SOLUTION | 500 mg | INTRAVENOUS | NDA | 29 sections |
Imipenem and Cilastatin | HUMAN PRESCRIPTION DRUG LABEL | 2 | 44567-705 | INJECTION, POWDER, FOR SOLUTION | 500 mg | INTRAVENOUS | ANDA | 24 sections |
Imipenem and Cilastatin | HUMAN PRESCRIPTION DRUG LABEL | 2 | 44567-705 | INJECTION, POWDER, FOR SOLUTION | 500 mg | INTRAVENOUS | ANDA | 24 sections |
Imipenem and Cilastatin | HUMAN PRESCRIPTION DRUG LABEL | 2 | 63323-322 | INJECTION, POWDER, FOR SOLUTION | 500 mg | INTRAVENOUS | ANDA | 26 sections |
Imipenem and Cilastatin | HUMAN PRESCRIPTION DRUG LABEL | 2 | 63323-322 | INJECTION, POWDER, FOR SOLUTION | 500 mg | INTRAVENOUS | ANDA | 26 sections |
Imipenem and Cilastatin | HUMAN PRESCRIPTION DRUG LABEL | 2 | 63323-322 | INJECTION, POWDER, FOR SOLUTION | 500 mg | INTRAVENOUS | ANDA | 26 sections |
Imipenem and Cilastatin | HUMAN PRESCRIPTION DRUG LABEL | 2 | 63323-349 | INJECTION, POWDER, FOR SOLUTION | 250 mg | INTRAVENOUS | ANDA | 26 sections |
Imipenem and Cilastatin | HUMAN PRESCRIPTION DRUG LABEL | 2 | 63323-349 | INJECTION, POWDER, FOR SOLUTION | 250 mg | INTRAVENOUS | ANDA | 26 sections |
Imipenem and Cilastatin | HUMAN PRESCRIPTION DRUG LABEL | 2 | 63323-349 | INJECTION, POWDER, FOR SOLUTION | 250 mg | INTRAVENOUS | ANDA | 26 sections |