Lactams, Macrocyclic

LACTAMS forming compounds with a ring size of approximately 1-3 dozen atoms.
DrugDrug NameDrug Indication
DB00615RifabutinFor the prevention of disseminated Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection.
DB01045RifampicinFor the treatment of Tuberculosis and Tuberculosis-related mycobacterial infections.
DB01201RifapentineFor the treatment of pulmonary tuberculosis.
DB01220RifaximinRifaximin has multiple indications by the FDA: for the treatment of patients (≥12 years of age) with traveller's diarrhea caused by noninvasive strains of Escherichia coli; for the reduction of overt hepatic encephalopathy recurrence in patients ≥18 years of age; and in May 2015 it was approved for irritable bowel syndrome with diarrhea (IBS-D) treatment in adult men and women.
DB04934RifalazilInvestigated for use/treatment in atherosclerosis, bacterial infection, and peripheral vascular disease.
DB05773Trastuzumab emtansineUsed in HER2-positive, metastatic breast cancer patients who have already used taxane and/or trastuzumab for metastatic disease or had their cancer recur within 6 months of adjuvant treatment.
DB06318AVE9633Investigated for use/treatment in leukemia (myeloid).
DB06342Coltuximab ravtansineInvestigated for use/treatment in lymphoma (non-hodgkin's).
DB12089Lorvotuzumab mertansineNot Available
DB12489Mirvetuximab SoravtansineNot Available
DB04220CGP 4832Not Available
DB11753RifamycinRifamycin is indicated for the treatment of adult patients with travelers' diarrhea caused by noninvasive strains of _E. coli_. The status of the disease should not be complicated by fever or blood in the stool. To prevent drug-resistant bacteria, it is important to mention that the use of rifamycin for this indication should be only done in cases where the infection is proven or strongly suspected to be caused by bacteria.[L4802] Travallers' diarrhea is very common problem affecting 20-60% of the travellers and it is defined as an increase in frequency of bowel movements to three or more loose stools per day during a trip abroad. This condition is rarely life threatening but in severe cases it can produce dehydration and sepsis. The most common cause of travellers' diarrhea is a pathogen and from the pathogens identified, bacteria is the most common cause followed by norovirus, rotavirus and similar viruses.[A39995]
DB14809Anetumab ravtansineNot Available
DB1521325-desacetylrifapentineNot Available
DrugDrug NameTargetType
DB00615RifabutinDNA-directed RNA polymerase subunit alphatarget
DB00615RifabutinHeat shock protein HSP 90-alphatarget
DB00615RifabutinEndoplasmintarget
DB00615RifabutinCytochrome P450 3A4enzyme
DB00615RifabutinDNA-directed RNA polymerase subunit betatarget
DB00615RifabutinDNA-directed RNA polymerase subunit beta'target
DB00615RifabutinCytochrome P450 2C19enzyme
DB00615RifabutinCytochrome P450 2B6enzyme
DB00615RifabutinCytochrome P450 2C8enzyme
DB00615RifabutinCytochrome P450 2C9enzyme
DB00615RifabutinCytochrome P450 2D6enzyme
DB00615RifabutinMultidrug resistance protein 1transporter
DB01045RifampicinDNA-directed RNA polymerase subunit betatarget
DB01045RifampicinNuclear receptor subfamily 1 group I member 2target
DB01045RifampicinCytochrome P450 3A4enzyme
DB01045RifampicinCytochrome P450 1A2enzyme
DB01045RifampicinCytochrome P450 2C8enzyme
DB01045RifampicinUDP-glucuronosyltransferase 1-1enzyme
DB01045RifampicinCytochrome P450 2C9enzyme
DB01045RifampicinCytochrome P450 2B6enzyme
DB01045RifampicinCytochrome P450 2C19enzyme
DB01045RifampicinCanalicular multispecific organic anion transporter 2transporter
DB01045RifampicinMultidrug resistance-associated protein 5transporter
DB01045RifampicinMultidrug resistance protein 1transporter
DB01045RifampicinCanalicular multispecific organic anion transporter 1transporter
DB01045RifampicinSolute carrier organic anion transporter family member 2B1transporter
DB01045RifampicinBile salt export pumptransporter
DB01045RifampicinMultidrug resistance-associated protein 1transporter
DB01045RifampicinSolute carrier organic anion transporter family member 1A2transporter
DB01045RifampicinSolute carrier organic anion transporter family member 1B3transporter
DB01045RifampicinSolute carrier family 22 member 7transporter
DB01045RifampicinSolute carrier organic anion transporter family member 1B1transporter
DB01045RifampicinDNA-directed RNA polymerase subunit beta'target
DB01045RifampicinCytochrome P450 2A6enzyme
DB01045RifampicinCytochrome P450 2E1enzyme
DB01045RifampicinCytochrome P450 3A43enzyme
DB01045RifampicinCytochrome P450 3A7enzyme
DB01045RifampicinCytochrome P450 4A11enzyme
DB01045RifampicinSolute carrier organic anion transporter family member 1B1target
DB01045RifampicinSolute carrier organic anion transporter family member 1A2target
DB01045RifampicinSolute carrier organic anion transporter family member 1B3target
DB01045RifampicinLanosterol 14-alpha demethylasetarget
DB01045RifampicinSerum albumintarget
DB01045RifampicinSolute carrier organic anion transporter family member 2B1target
DB01045RifampicinCytochrome P450 2D6enzyme
DB01045RifampicinSolute carrier family 22 member 6transporter
DB01045RifampicinSolute carrier family 22 member 8transporter
DB01045RifampicinUDP-glucuronosyltransferase 1A9enzyme
DB01201RifapentineDNA-directed RNA polymerase subunit beta'target
DB01201RifapentineCytochrome P450 2C8enzyme
DB01201RifapentineCytochrome P450 2C9enzyme
DB01201RifapentineCytochrome P450 3A4enzyme
DB01201RifapentineCytochrome P450 2D6enzyme
DB01201RifapentineCytochrome P450 3A43enzyme
DB01201RifapentineCytochrome P450 2C19enzyme
DB01201RifapentineCytochrome P450 2B6enzyme
DB01220RifaximinDNA-directed RNA polymerase subunit betatarget
DB01220RifaximinNuclear receptor subfamily 1 group I member 2target
DB01220RifaximinCytochrome P450 3A4enzyme
DB01220RifaximinCytochrome P450 2C19enzyme
DB01220RifaximinCytochrome P450 2C8enzyme
DB01220RifaximinCytochrome P450 2D6enzyme
DB04934RifalazilDNA-directed RNA polymerase subunit betatarget
DB04934RifalazilCytochrome P450 3A4enzyme
DB05773Trastuzumab emtansineReceptor tyrosine-protein kinase erbB-2target
DB05773Trastuzumab emtansineMultidrug resistance protein 1transporter
DB05773Trastuzumab emtansineCytochrome P450 3A4enzyme
DB05773Trastuzumab emtansineCytochrome P450 3A5enzyme
DB06318AVE9633Myeloid cell surface antigen CD33target
DB06318AVE9633Cytochrome P450 3A4enzyme
DB06342Coltuximab ravtansineB-lymphocyte antigen CD19target
DB06342Coltuximab ravtansineCytochrome P450 3A4enzyme
DB12089Lorvotuzumab mertansineCytochrome P450 3A4enzyme
DB12489Mirvetuximab SoravtansineCytochrome P450 3A4enzyme
DB04220CGP 4832Ferrichrome-iron receptortarget
DB11753RifamycinCytochrome P450 3A4enzyme
DB11753RifamycinCytochrome P450 2C19enzyme
DB11753RifamycinCytochrome P450 2B6enzyme
DB11753RifamycinCytochrome P450 2C8enzyme
DB11753RifamycinCytochrome P450 2C9enzyme
DB11753RifamycinCytochrome P450 2D6enzyme
DB11753RifamycinSolute carrier organic anion transporter family member 1A2transporter
DB11753RifamycinSolute carrier organic anion transporter family member 1B1transporter
DB11753RifamycinSolute carrier organic anion transporter family member 1B3transporter
DB11753RifamycinSolute carrier organic anion transporter family member 2A1transporter
DB11753RifamycinSolute carrier organic anion transporter family member 2B1transporter
DB11753RifamycinSerum albumincarrier
DB11753RifamycinDNA-directed RNA polymerase subunit betatarget
DB11753RifamycinDNA-directed RNA polymerase subunit alphatarget
DB11753RifamycinDNA-directed RNA polymerase subunit beta'target
DB11753RifamycinMultidrug and toxin extrusion protein 1transporter
DB11753RifamycinCytochrome P450 1A2enzyme
DB11753RifamycinMultidrug resistance protein 1transporter