ceftolozane 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antibiotics, cefalosporanic acid derivatives | 4922 | 689293-68-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Ceftolozane belongs to the cephalosporin class of antibacterial drugs. The bactericidal action of ceftolozane results from inhibition of cell wall biosynthesis, and is mediated through binding to penicillin-binding proteins (PBPs). Ceftolozane is an inhibitor of PBPs of P. aeruginosa (e.g., PBP1b, PBP1c, and PBP3) and E. coli (e.g., PBP3).
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 3 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Hosey CM, Chan R, Benet LZ |
| Vd (Volume of distribution) | 0.17 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.16 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.81 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 2.58 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 18, 2015 | EMA | MERCK SHARP & DOHME B.V. | |
| Dec. 19, 2014 | FDA | CUBIST PHARMS | |
| Jan. 8, 2019 | PMDA | MSD K.K. |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J01DI54 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER BETA-LACTAM ANTIBACTERIALS Other cephalosporins and penems |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000892 | Anti-Infective Agents, Urinary |
| MeSH PA | D065093 | beta-Lactamase Inhibitors |
| MeSH PA | D004791 | Enzyme Inhibitors |
| FDA CS | M0003827 | Cephalosporins |
| FDA EPC | N0000175488 | Cephalosporin Antibacterial |
| CHEBI has role | CHEBI:33281 | antibiotics |
| CHEBI has role | CHEBI:35441 | antiinfective agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Abscess of liver | indication | 27916005 | |
| Acute pyelonephritis | indication | 36689008 | DOID:559 |
| Urinary tract infectious disease | indication | 68566005 | |
| Haemophilus influenzae pneumonia | indication | 70036007 | |
| Abdominal abscess | indication | 75100008 | |
| Cholecystitis | indication | 76581006 | DOID:1949 |
| Infectious disease of abdomen | indication | 128070006 | |
| Bacterial peritonitis | indication | 197171003 | |
| Bacterial cystitis | indication | 424551004 | |
| Nosocomial pneumonia | indication | 425464007 | |
| Ventilator-acquired pneumonia | indication | 429271009 | |
| Sepsis caused by Haemophilus influenzae | indication | 447685007 | |
| Sepsis caused by Serratia | indication | 449084002 | |
| Bacterial pyelonephritis | indication | 838353009 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 2.97 | acidic |
| pKa2 | 3.5 | acidic |
| pKa3 | 11.54 | acidic |
| pKa4 | 12.82 | acidic |
| pKa5 | 13.65 | acidic |
| pKa6 | 9.85 | Basic |
| pKa7 | 4.05 | Basic |
| pKa8 | 0.73 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 7129232 | May 15, 2028 | COMPLICATED INTRA-ABDOMINAL INFECTIONS (CIAI), USED IN COMBINATION WITH METRONIDAZOLE, IN ADULT AND PEDIATRIC PATIENTS (BIRTH TO LESS THAN 18 YEARS OF AGE) |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 7129232 | May 15, 2028 | COMPLICATED URINARY TRACT INFECTIONS (CUTI), INCLUDING PYELONEPHRITIS, IN ADULT AND PEDIATRIC PATIENTS (BIRTH TO LESS THAN 18 YEARS OLD) |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 7129232 | May 15, 2028 | METHODS FOR TREATING BACTERIAL INFECTIONS |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 7129232 | May 15, 2028 | METHODS OF TREATING BACTERIAL ILLNESSES |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 10028963 | Sept. 7, 2032 | TREATMENT OF HOSPITAL-ACQUIRED BACTERIAL PNEUMONIA |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 10028963 | Sept. 7, 2032 | TREATMENT OF VENTILATOR-ASSOCIATED BACTERIAL PNEUMONIA |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 9724353 | Sept. 7, 2032 | TREATMENT OF HOSPITAL-ACQUIRED BACTERIAL PNEUMONIA |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 9724353 | Sept. 7, 2032 | TREATMENT OF VENTILATOR-ASSOCIATED BACTERIAL PNEUMONIA |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 8685957 | Sept. 27, 2032 | METHODS OF TREATING BACTERIAL ILLNESSES |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 10420841 | March 14, 2034 | COMPLICATED INTRA-ABDOMINAL INFECTIONS (CIAI), USED IN COMBINATION WITH METRONIDAZOLE, IN ADULT AND PEDIATRIC PATIENTS (BIRTH TO LESS THAN 18 YEARS OF AGE) |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 10420841 | March 14, 2034 | COMPLICATED URINARY TRACT INFECTIONS (CUTI), INCLUDING PYELONEPHRITIS, IN ADULT AND PEDIATRIC PATIENTS (BIRTH TO LESS THAN 18 YEARS OLD) |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 10420841 | March 14, 2034 | TREATMENT OF COMPLICATED INTRA-ABDOMINAL INFECTION |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 10420841 | March 14, 2034 | TREATMENT OF COMPLICATED URINARY TRACT INFECTION |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 11278622 | March 14, 2034 | TREATMENT OF HOSPITAL-ACQUIRED BACTERIAL PNEUMONIA (HABP) |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 11278622 | March 14, 2034 | TREATMENT OF VENTILATOR-ASSOCIATED BACTERIAL PNEUMONIA (VABP) |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 8968753 | March 14, 2034 | COMPLICATED INTRA-ABDOMINAL INFECTIONS (CIAI), USED IN COMBINATION WITH METRONIDAZOLE, IN ADULT AND PEDIATRIC PATIENTS (BIRTH TO LESS THAN 18 YEARS OF AGE) |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 8968753 | March 14, 2034 | COMPLICATED URINARY TRACT INFECTIONS (CUTI), INCLUDING PYELONEPHRITIS, IN ADULT AND PEDIATRIC PATIENTS (BIRTH TO LESS THAN 18 YEARS OLD) |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 8968753 | March 14, 2034 | TREATMENT OF COMPLICATED INTRA-ABDOMINAL INFECTION |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 8968753 | March 14, 2034 | TREATMENT OF COMPLICATED URINARY TRACT INFECTION, INCLUDING PYELONEPHRITIS |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 10376496 | Sept. 9, 2034 | TREATMENT OF COMPLICATED INTRA-ABDOMINAL INFECTION IN PATIENTS WITH END-STAGE RENAL DISEASE ON HEMODIALYSIS |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 10376496 | Sept. 9, 2034 | TREATMENT OF COMPLICATED URINARY TRACT INFECTION IN PATIENTS WITH END-STAGE RENAL DISEASE ON HEMODIALYSIS |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 10933053 | Sept. 9, 2034 | TREATMENT OF HOSPITAL-ACQUIRED BACTERIAL PNEUMONIA IN PATIENTS WITH END-STAGE RENAL DISEASE ON HEMODIALYSIS |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | 10933053 | Sept. 9, 2034 | TREATMENT OF VENTILATOR-ASSOCIATED BACTERIAL PNEUMONIA IN PATIENTS WITH END-STAGE RENAL DISEASE ON HEMODIALYSIS |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | Dec. 19, 2019 | NEW CHEMICAL ENTITY |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | Dec. 19, 2024 | GENERATING ANTIBIOTIC INCENTIVES NOW |
| EQ 1GM BASE/VIAL;EQ 0.5GM BASE/VIAL | ZERBAXA | CUBIST PHARMS LLC | N206829 | Dec. 19, 2014 | RX | POWDER | INTRAVENOUS | April 21, 2025 | NEW PATIENT POPULATION |
Bioactivity Summary:
None
External reference:
| ID | Source |
|---|---|
| 37A4IES95Q | UNII |
| D10097 | KEGG_DRUG |
| 4034036 | VUID |
| N0000191292 | NUI |
| 936111-69-2 | SECONDARY_CAS_RN |
| 4034035 | VANDF |
| 4034036 | VANDF |
| C3852726 | UMLSCUI |
| CHEBI:134719 | CHEBI |
| CHEMBL2103872 | ChEMBL_ID |
| 53234134 | PUBCHEM_CID |
| DB09050 | DRUGBANK_ID |
| CHEMBL1213250 | ChEMBL_ID |
| 9426 | INN_ID |
| C519491 | MESH_SUPPLEMENTAL_RECORD_UI |
| C000594038 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10788 | IUPHAR_LIGAND_ID |
| 1597608 | RXNORM |
| 231579 | MMSL |
| 30783 | MMSL |
| d08325 | MMSL |
| 015822 | NDDF |
| 015823 | NDDF |
| 708792003 | SNOMEDCT_US |
| 734470005 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| ZERBAXA | HUMAN PRESCRIPTION DRUG LABEL | 2 | 67919-030 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 1 g | INTRAVENOUS | NDA | 28 sections |
| ZERBAXA | HUMAN PRESCRIPTION DRUG LABEL | 2 | 67919-030 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 1 g | INTRAVENOUS | NDA | 28 sections |
| ZERBAXA | HUMAN PRESCRIPTION DRUG LABEL | 2 | 67919-030 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 1 g | INTRAVENOUS | NDA | 28 sections |