Macrolides

A group of often glycosylated macrocyclic compounds formed by chain extension of multiple PROPIONATES cyclized into a large (typically 12, 14, or 16)-membered lactone. Macrolides belong to the POLYKETIDES class of natural products, and many members exhibit ANTIBIOTIC properties.
DrugDrug NameDrug Indication
DB00199Erythromycin Erythromycin is indicated in the treatment of infections caused by susceptible strains of the designated organisms in the diseases listed below [FDA label]: _Respiratory infections_ **Upper respiratory tract infections** of mild to moderate degree caused by Streptococcus pyogenes, Streptococcus pneumoniae, or Haemophilus influenzae (when used concomitantly with adequate doses of sulfonamides, since many strains of H. influenzae are not susceptible to the erythromycin concentrations ordinarily achieved) [FDA label]. **Lower-respiratory tract infections** of mild to moderate severity caused by Streptococcus pneumoniae or Streptococcus pyogenes. Listeriosis caused by Listeria monocytogenes [FDA label]. **Pertussis (whooping cough)** caused by Bordetella pertussis. Erythromycin is effective in eliminating the organism from the nasopharynx of infected individuals rendering them noninfectious. Some clinical studies suggest that erythromycin may be helpful in the prophylaxis of pertussis in exposed susceptible individuals [FDA label]. **Respiratory tract infections** due to Mycoplasma pneumoniae [FDA label]. **Legionnaires’ Disease** caused by Legionella pneumophila. Although no controlled clinical efficacy studies have been conducted, in vitro and limited preliminary clinical data suggest that erythromycin may be effective in treating Legionnaires’ Disease [FDA label]. **Diphtheria**: Infections due to Corynebacterium diphtheriae, as an adjunct to antitoxin, to prevent establishment of carriers and to eradicate the organism in carriers [FDA label]. _Skin infections_ **Skin and skin structure infections** of mild to moderate severity caused by Streptococcus pyogenes or Staphylococcus aureus (resistant staphylococci may emerge during treatment) [FDA label]. **Erythrasma**: In the treatment of infections due to Corynebacterium minutissimum [FDA label]. _Gastrointestinal infections_ **Intestinal amebiasis** caused by Entamoeba histolytica (oral erythromycins only). Extraenteric amebiasis requires treatment with other agents [FDA label]. _Genital infections/STIs_ **Acute pelvic inflammatory disease** caused by Neisseria gonorrhoeae: As an alternative drug in treatment of acute pelvic inflammatory disease caused by N. gonorrhoeae in female patients with a history of sensitivity to penicillin. Patients should have a serologic test for syphilis before receiving erythromycin as treatment of gonorrhea and a follow-up serologic test for syphilis after 3 months [FDA label]. **Syphilis** caused by Treponema pallidum: Erythromycin is an alternate choice of treatment for primary syphilis in patients allergic to the penicillins. In treatment of primary syphilis, spinal fluid examinations should be done before treatment and as part of follow-up after therapy [FDA label]. **Chlamydia trachomatis**: conjunctivitis of the newborn, pneumonia of infancy, and urogenital infections during pregnancy. When tetracyclines are contraindicated or not tolerated, erythromycin is indicated for the treatment of uncomplicated urethral, endocervical, or rectal infections in adults due to Chlamydia trachomatis [FDA label]. **Nongonnoconnal urethritis**: When tetracyclines are contraindicated or not tolerated, erythromycin is indicated for the treatment of nongonococcal urethritis caused by Ureaplasma urealyticum [FDA label].
DB00778RoxithromycinUsed to treat respiratory tract, urinary and soft tissue infections.
DB01321JosamycinFor the treatment of bacterial infections.
DB00954DirithromycinFor the treatment of the following mild-to-moderate infections caused by susceptible strains of microorganisms: acute bacterial exacerbations of chronic bronchitis, secondary bacterial infection of acute bronchitis, community-acquired pneumonia, pharyngitis/tonsilitis, and uncomplicated skin and skin structure infections.
DB00976TelithromycinFor the treatment of Pneumococcal infection, acute sinusitis, acute bacterial tonsillitis, acute bronchitis and bronchiolitis, lower respiratory tract infection and lobar (pneumococcal) pneumonia.
DB08874FidaxomicinTreatment of Clostridium difficile-associated diarrhea
DB09308SolithromycinInvestigated for the treatment of community-acquired pneumonia (CAP).
DB13179TroleandomycinFor the treatment of bacterial infection.
DB13287MiocamycinNot Available
DB13338FlurithromycinNot Available
DB13409RokitamycinNot Available
DB13456MidecamycinMidecamycin was used for the treatment of infections in the oral cavity, upper and lower respiratory tracts and skin and soft tissue infections. The alone use of midecamycin was mainly used in Europe or Japan.[T207]
DB06145SpiramycinMacrolide antibiotic for treatment of various infections.
DB00207AzithromycinAzithromycin should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria in order to prevent the development antimicrobial resistance and maintain the efficacy of azithromycin [FDA label]. Azithromycin is indicated for the treatment of patients with mild to moderate infections caused by susceptible strains of the microorganisms listed in the specific conditions below. Recommended dosages, duration of therapy and considerations for various patient populations may vary among these infections. Refer to the FDA label and "Indications" section of this drug entry for detailed information [FDA label]. **Adults**: Acute bacterial exacerbations of chronic obstructive pulmonary disease due to _Haemophilus influenzae_, _Moraxella catarrhalis_ or _Streptococcus pneumoniae_ Acute bacterial sinusitis due to _Haemophilus influenzae_, _Moraxella catarrhalis_ or _Streptococcus pneumoniae_ Community-acquired pneumonia due to _Chlamydophila pneumoniae_, _Haemophilus influenzae_, _Mycoplasma pneumoniae_ or _Streptococcus pneumoniae_ in patients appropriate for oral therapy Pharyngitis/tonsillitis caused by _Streptococcus pyogenes_ as an alternative to first-line therapy in individuals who cannot use first-line therapy. Uncomplicated skin and skin structure infections due to _Staphylococcus aureus_, _Streptococcus pyogenes_, or _Streptococcus agalactiae_. Abscesses usually require surgical drainage. Urethritis and cervicitis due to _Chlamydia trachomatis_ or _Neisseria gonorrhoeae_. Genital ulcer disease in men due to _Haemophilus ducreyi_ (chancroid). Due to the small number of women included in clinical trials, the efficacy of azithromycin in the treatment of chancroid in women has not been established. **Pediatric Patients** Acute otitis media caused by _Haemophilus influenzae_, _Moraxella catarrhalis_ or _Streptococcus pneumoniae_ Community-acquired pneumonia due to _Chlamydophila pneumoniae_, _Haemophilus influenzae_, _Mycoplasma pneumoniae_ or _Streptococcus pneumoniae_ in patients appropriate for oral therapy. Pharyngitis/tonsillitis caused by _Streptococcus pyogenes_ as an alternative to first-line therapy in individuals who cannot use first-line therapy.
DB01152CandicidinUsed in the topical treatment of vulvovaginal candidiasis.
DB01211ClarithromycinAn alternative medication for the treatment of acute otitis media caused by H. influenzae, M. catarrhalis, or S. pneumoniae in patients with a history of type I penicillin hypersensitivity. Also for the treatment of pharyngitis and tonsillitis caused by susceptible Streptococcus pyogenes, as well as respiratory tract infections including acute maxillary sinusitis, acute bacterial exacerbations of chronic bronchitis, mild to moderate community-acquired pneuomia, Legionnaires' disease, and pertussis. Other indications include treatment of uncomplicated skin or skin structure infections, helicobacter pylori infection, duodenal ulcer disease, bartonella infections, early Lyme disease, and encephalitis caused by Toxoplasma gondii (in HIV infected patients in conjunction with pyrimethamine). Clarithromycin may also decrease the incidence of cryptosporidiosis, prevent the occurence of α-hemolytic (viridans group) streptococcal endocarditis, as well as serve as a primary prevention for Mycobacterium avium complex (MAC) bacteremia or disseminated infections (in adults, adolescents, and children with advanced HIV infection).
DB01590EverolimusEverolimus is indicated for the treatment of postmenopausal women with advanced hormone receptor-positive, HER2-negative breast cancer (advanced HR+ BC) in combination with exemestane, after failure of treatment with letrozole or anastrozole. Indicated for the treatment of adult patients with progressive neuroendocrine tumors of pancreatic origin (PNET) with unresectable, locally advanced or metastatic disease. Indicated for the treatment of adult patients with advanced renal cell carcinoma (RCC) after failure of treatment with sunitinib or sorafenib. Indicated for the treatment of adult patients with renal angiomyolipoma and tuberous sclerosis complex (TSC), not requiring immediate surgery. Indicated in pediatric and adult patients with tuberous sclerosis complex (TSC) for the treatment of subependymal giant cell astrocytoma (SEGA) that requires therapeutic intervention but cannot be curatively resected.
DB01873Epothilone DInvestigated for use/treatment in colorectal cancer, lung cancer, breast cancer, solid tumors, and prostate cancer.
DB03010PatupiloneInvestigated for use/treatment in ovarian cancer, lung cancer, brain cancer, breast cancer, and gastric cancer.
DB040706-Deoxyerythronolide BNot Available
DB04845IxabepiloneInvestigated for use/treatment in breast cancer, head and neck cancer, melanoma, lung cancer, lymphoma (non-hodgkin's), prostate cancer, renal cell carcinoma, and cancer/tumors (unspecified).
DB05903KOS-1584Investigated for use/treatment in solid tumors.
DB06233RidaforolimusInvestigated for use/treatment in solid tumors, sarcoma, cancer/tumors (unspecified), endometrial cancer, prostate cancer, and bone metastases.
DB06287TemsirolimusFor the treatment of renal cell carcinoma (RCC). Also investigated for use/treatment in breast cancer, lymphoma (unspecified), rheumatoid arthritis, and multiple myeloma.
DB06318AVE9633Investigated for use/treatment in leukemia (myeloid).
DB06342Coltuximab ravtansineInvestigated for use/treatment in lymphoma (non-hodgkin's).
DB06419CethromycinInvestigated for use/treatment in bacterial infection, pediatric indications, and pneumonia.
DB06587MitemcinalInvestigated for use/treatment in gastroparesis and irritable bowel syndrome (IBS).
DB07348Brefeldin ANot Available
DB09309KitasamycinNot Available
DB11383CarbomycinNot Available
DB11400DoramectinNot Available
DB11405EprinomectinNot Available
DB11442OleandomycinNot Available
DB11459SelamectinNot Available
DB11470TildipirosinNot Available
DB11471TilmicosinNot Available
DB11475TylosinNot Available
DB11554TylvalosinNot Available
DB11752Bryostatin 1Not Available
DB12089Lorvotuzumab mertansineNot Available
DB12266EpofolateNot Available
DB12391SagopiloneNot Available
DB12489Mirvetuximab SoravtansineNot Available
DB13633MepartricinNot Available
DB00877SirolimusFor the prophylaxis of organ rejection in patients receiving renal transplants.
DB14809Anetumab ravtansineNot Available
DrugDrug NameTargetType
DB00199Erythromycin23S rRNAtarget
DB00199ErythromycinCytochrome P450 3A4enzyme
DB00199ErythromycinCytochrome P450 3A7enzyme
DB00199ErythromycinMultidrug resistance protein 1transporter
DB00199ErythromycinSolute carrier organic anion transporter family member 1B1transporter
DB00199ErythromycinMotilin receptortarget
DB00199ErythromycinPotassium voltage-gated channel subfamily H member 2target
DB00199ErythromycinCytochrome P450 3A5enzyme
DB00199ErythromycinSolute carrier organic anion transporter family member 1B3transporter
DB00199ErythromycinBile salt export pumptransporter
DB00199ErythromycinBacterial 50S Ribosomal Subunittarget
DB00199ErythromycinCanalicular multispecific organic anion transporter 1transporter
DB00199ErythromycinSolute carrier organic anion transporter family member 1A2transporter
DB00778Roxithromycin50S ribosomal protein L10target
DB00778RoxithromycinMultidrug resistance protein 1target
DB00778RoxithromycinCytochrome P450 3A4enzyme
DB00778RoxithromycinCytochrome P450 2B6enzyme
DB01321Josamycin50S ribosomal protein L4target
DB01321JosamycinCytochrome P450 3A4enzyme
DB00954Dirithromycin23S rRNAtarget
DB00954DirithromycinCytochrome P450 3A4enzyme
DB00976Telithromycin23S rRNAtarget
DB00976TelithromycinCytochrome P450 3A4enzyme
DB00976TelithromycinCytochrome P450 3A5enzyme
DB00976TelithromycinCytochrome P450 3A7enzyme
DB00976TelithromycinSolute carrier organic anion transporter family member 1B1transporter
DB00976TelithromycinSolute carrier organic anion transporter family member 1B3transporter
DB08874FidaxomicinMultidrug resistance protein 1transporter
DB08874FidaxomicinRNA polymerase sigma factortarget
DB08874FidaxomicinCytochrome P450 3A4enzyme
DB09308SolithromycinCytochrome P450 3A4enzyme
DB13179TroleandomycinCytochrome P450 2C9enzyme
DB13179TroleandomycinCytochrome P450 3A5enzyme
DB13179TroleandomycinCytochrome P450 3A43enzyme
DB13179Troleandomycin50S ribosomal protein L4target
DB13179Troleandomycin50S ribosomal protein L32target
DB13179TroleandomycinMultidrug resistance protein 1transporter
DB13179TroleandomycinCytochrome P450 2C18enzyme
DB13179TroleandomycinCytochrome P450 2C8enzyme
DB13179TroleandomycinCytochrome P450 3A4enzyme
DB13179TroleandomycinNuclear receptor subfamily 1 group I member 2target
DB13179TroleandomycinCytochrome P450 3A7enzyme
DB13287MiocamycinCytochrome P450 3A4enzyme
DB13338FlurithromycinCytochrome P450 3A4enzyme
DB13409RokitamycinCytochrome P450 3A4enzyme
DB13456MidecamycinCytochrome P450 3A4enzyme
DB06145SpiramycinCytochrome P450 3A4enzyme
DB06145Spiramycin50S ribosomal protein L3target
DB00207Azithromycin23S rRNAtarget
DB00207AzithromycinMultidrug resistance protein 1transporter
DB00207AzithromycinCytochrome P450 3A4enzyme
DB00207AzithromycinProtein-arginine deiminase type-4target
DB00207AzithromycinCanalicular multispecific organic anion transporter 1transporter
DB00207AzithromycinBacterial 50S Ribosomal Subunittarget
DB01152CandicidinErgosteroltarget
DB01152CandicidinCytochrome P450 3A4enzyme
DB01211Clarithromycin50S ribosomal protein L10target
DB01211ClarithromycinCytochrome P450 3A4enzyme
DB01211ClarithromycinCytochrome P450 2C19enzyme
DB01211ClarithromycinCytochrome P450 3A5enzyme
DB01211ClarithromycinCytochrome P450 3A7enzyme
DB01211ClarithromycinMultidrug resistance protein 1transporter
DB01211ClarithromycinSolute carrier family 22 member 7transporter
DB01211ClarithromycinPotassium voltage-gated channel subfamily H member 2target
DB01211ClarithromycinSolute carrier organic anion transporter family member 1B1target
DB01211ClarithromycinSolute carrier organic anion transporter family member 1B3target
DB01211ClarithromycinBile salt export pumptransporter
DB01590EverolimusSerine/threonine-protein kinase mTORtarget
DB01590EverolimusCytochrome P450 3A4enzyme
DB01590EverolimusSolute carrier organic anion transporter family member 1B1transporter
DB01590EverolimusSolute carrier organic anion transporter family member 1B3transporter
DB01590EverolimusSolute carrier organic anion transporter family member 1A2transporter
DB01873Epothilone DTubulin alpha-3C/D chaintarget
DB01873Epothilone DTubulin beta chaintarget
DB01873Epothilone DTubulin beta-1 chaintarget
DB01873Epothilone DTubulin beta-4B chaintarget
DB01873Epothilone DTubulin beta-4A chaintarget
DB01873Epothilone DTubulin alpha-4A chaintarget
DB01873Epothilone DTubulin beta-3 chaintarget
DB01873Epothilone DTubulin alpha-1C chaintarget
DB01873Epothilone DTubulin alpha-8 chaintarget
DB01873Epothilone DTubulin alpha-1B chaintarget
DB01873Epothilone DTubulin alpha-1A chaintarget
DB01873Epothilone DCytochrome P450 3A4enzyme
DB03010PatupiloneTubulin alpha-3C/D chaintarget
DB03010PatupiloneTubulin beta chaintarget
DB03010PatupiloneTubulin beta-1 chaintarget
DB03010PatupiloneTubulin beta-4B chaintarget
DB03010PatupiloneTubulin beta-4A chaintarget
DB03010PatupiloneTubulin alpha-4A chaintarget
DB03010PatupiloneTubulin beta-3 chaintarget
DB03010PatupiloneTubulin alpha-1C chaintarget
DB03010PatupiloneTubulin alpha-8 chaintarget
DB03010PatupiloneTubulin alpha-1B chaintarget
DB03010PatupiloneTubulin alpha-1A chaintarget
DB03010PatupiloneCytochrome P450 3A4enzyme
DB040706-Deoxyerythronolide B6-deoxyerythronolide B hydroxylasetarget
DB040706-Deoxyerythronolide BCytochrome P450 3A4enzyme
DB04845IxabepiloneTubulin beta-3 chaintarget
DB04845IxabepiloneCytochrome P450 3A4enzyme
DB05903KOS-1584Cytochrome P450 3A4enzyme
DB06233RidaforolimusSerine/threonine-protein kinase mTORtarget
DB06233RidaforolimusCytochrome P450 3A4enzyme
DB06287TemsirolimusSerine/threonine-protein kinase mTORtarget
DB06287TemsirolimusCytochrome P450 3A4enzyme
DB06287TemsirolimusCytochrome P450 3A5enzyme
DB06287TemsirolimusCytochrome P450 3A7enzyme
DB06287TemsirolimusCytochrome P450 2D6enzyme
DB06287TemsirolimusMultidrug resistance protein 1transporter
DB06318AVE9633Myeloid cell surface antigen CD33target
DB06318AVE9633Cytochrome P450 3A4enzyme
DB06342Coltuximab ravtansineB-lymphocyte antigen CD19target
DB06342Coltuximab ravtansineCytochrome P450 3A4enzyme
DB06419Cethromycin23S rRNAtarget
DB06419CethromycinCytochrome P450 3A5enzyme
DB06419CethromycinCytochrome P450 3A4enzyme
DB06587MitemcinalMotilin receptortarget
DB06587MitemcinalCytochrome P450 3A4enzyme
DB07348Brefeldin ACytohesin-2target
DB07348Brefeldin AADP-ribosylation factor 1target
DB07348Brefeldin ACytochrome P450 3A4enzyme
DB09309KitasamycinCytochrome P450 3A4enzyme
DB11383CarbomycinCytochrome P450 3A4enzyme
DB11400DoramectinCytochrome P450 3A4enzyme
DB11405EprinomectinCytochrome P450 3A4enzyme
DB11442OleandomycinCytochrome P450 3A4enzyme
DB11459SelamectinCytochrome P450 3A4enzyme
DB11470TildipirosinCytochrome P450 3A4enzyme
DB11471TilmicosinCytochrome P450 3A4enzyme
DB11475TylosinCytochrome P450 3A4enzyme
DB11554TylvalosinCytochrome P450 3A4enzyme
DB11752Bryostatin 1Cytochrome P450 3A4enzyme
DB12089Lorvotuzumab mertansineCytochrome P450 3A4enzyme
DB12266EpofolateCytochrome P450 3A4enzyme
DB12391SagopiloneCytochrome P450 3A4enzyme
DB12489Mirvetuximab SoravtansineCytochrome P450 3A4enzyme
DB13633MepartricinCytochrome P450 3A4enzyme
DB00877SirolimusPeptidyl-prolyl cis-trans isomerase FKBP1Atarget
DB00877SirolimusCytochrome P450 3A4enzyme
DB00877SirolimusSerine/threonine-protein kinase mTORtarget
DB00877SirolimusFibroblast growth factor 2target
DB00877SirolimusCytochrome P450 3A5enzyme
DB00877SirolimusCytochrome P450 3A7enzyme
DB00877SirolimusMultidrug resistance protein 1transporter
DB00877SirolimusSolute carrier organic anion transporter family member 1B1transporter
DB00877SirolimusMultidrug and toxin extrusion protein 1transporter