- Omadacycline tosylate is a new tetracycline antibiotic in the pipeline, which can inhibit the 30s subunit of bacterial ribosome.
- Asmita Sapkota, .et al. , Biomed Pharmacother, 2024, Oct:179:117313 PMID: 39167844
- Xiaoming Liu, .et al. , J Antibiot (Tokyo), 2022, Aug;75(8):463-471 PMID: 35760902
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Protein synthesis inhibitor
Linezolid is a synthetic antibiotic used for the treatment of serious infections.- Carly Deusenbery, .et al. , ACS Infect Dis, 2023, Oct 13;9(10):1949-1963 PMID: 37646612
- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
- Zewen Wen, .et al. , J Antibiot (Tokyo), 2022, Sep;75(9):498-508 PMID: 35896611
- Meikle V, .et al. , Antimicrob Agents Chemother, 2018, Nov 12. pii: AAC.01846-18 PMID: 30420480
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Neuraminidase Inhibitor
Peramivir is a neuraminidase inhibitor, acting as a transition-state analogue inhibitor of influenza neuraminidase and thereby preventing new viruses from emerging from infected cells.- Daisuke Kato, .et al. , PLoS One, 2018, 13(7): e0200761 PMID: 30001430
- Yuuki Kurebayashi, .et al. , PLoS One, 2016, 11(5): e0156400 PMID: 27232333
- TMC207 is a first-in-class diarylquinoline compound with a novel mechanism of action, the inhibition of bacterial ATP synthase, and potent activity against drug-sensitive and drug-resistant TB.
- Daniel J Pfau, .et al. , Autophagy Rep, 2025, 4(1):2473765 PMID: 40265045
- Nabila Ismail, .et al. , bioRxiv, 2025, March 11
- Boatema Ofori-Anyinam, .et al. , Nat Commun, 2024, Nov 13;15(1):9792 PMID: 39537610
- Khomotso Mmakola, .et al. , Preprints, 2024, Sep 18
- Asmita Sapkota, .et al. , Biomed Pharmacother, 2024, Oct:179:117313 PMID: 39167844
- Thanh Quang Nguyen, .et al. , Microbiol Spectr, 2023, Jun 15;11(3):e0063123 PMID: 37158736
- Rubeshan Perumal, .et al. , Infect Drug Resist, 2023, May 9;16:2849-2859 PMID: 37193296
- Christian C Otum, .et al. , Sci Rep, 2023, Jun 6;13(1):9212 PMID: 37280265
- Thanh Quang Nguyen, .et al. , Antimicrob Agents Chemother, 2022, Dec 20;66(12):e0044822 PMID: 36321819
- Jinsheng Cui, .et al. , Mar Drugs, 2022, Jun 16;20(6):400 PMID: 35736203
- Bettina Schulthess, .et al. , Antimicrob Agents Chemother, 2022, May 17;66(5) PMID: 35420492
- Puyskens A, .et al. , Cell Host Microbe, 2019, Dec 23. pii: S1931-3128(19)30634-1 PMID: 31901518
- Belosludtsev KN, .et al. , Biochim Biophys Acta Biomembr, 2019, Jan;1861(1):288-297 PMID: 29920239
- Meikle V, .et al. , Antimicrob Agents Chemother, 2018, Nov 12. pii: AAC.01846-18 PMID: 30420480
- Belosludtsev KN, .et al. , Chem Biol Interact, 2018, Nov 26;299:8-14 PMID: 30496736
- Wu X, .et al. , Biochem Biophys Res Commun, 2018, Jan 1;495(1):267-272 PMID: 29107691
- Jichan Jang, .et al. , Antimicrob Agents Chemother, 2017, Jul; 61(7): e02637-16 PMID: 28416541
- Marco Fiorillo, .et al. , Aging (Albany NY), 2016, Aug; 8(8): 1593-1606 PMID: 27344270
- Alvaro A. Ordonez, .et al. , Antimicrob Agents Chemother, 2015, Jan; 59(1): 642-649 PMID: 25403669
- Ke Liu, .et al. , Drug Metab Dispos, 2014, May; 42(5): 863-866 PMID: 24513655
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HIV Protease Inhibitor
Saquinavir is a protease inhibitor. Proteases are enzymes that cleave protein molecules into smaller fragments. Saquinavir inhibits both HIV-1 and HIV-2 proteases.- Ernawati Arifin Giri-Rachman, .et al. , ACS Synth Biol, 2024, Feb 16; 13(2): 509-520 PMID: 38316139
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Capreomycin Sulfate is a cyclic peptide antibiotic and thought to inhibit protein synthesis by binding to the 70S ribosomal unit.
- Hazem F M Abdelaal, .et al. , NPJ Antimicrob Resist, 2024, Dec 16;2(1):49 PMID: 39843983
- Amphotericin B is a polyene antifungal antibiotic from Streptomyces sp. Amphotericin B induces K+ leakage, which is separate from its lethal action, as was demonstrated in human erythrocytes and is due to the inhibitory effect on the Na+/K+ pump.
- Ilker Kiliccioglu, .et al. , Appl Biochem Biotechnol, 2025, Aug 23 PMID: 40848211
- J Chen, .et al. , Biomater Sci, 2020, Jun 21;8(12):3430-3442 PMID: 32406432
- Brincidofovir is a prodrug of cidofovir. Conjugated to a lipid, the compound is designed to release cidofovir intracellularly, allowing for higher intracellular and lower plasma concentrations of cidofovir, effectively increasing its activity against dsDNA viruses, as well as oral bioavailability.
- Jason Yongsheng Chan, .et al. , Research Square, 2025, June 3rd
- Tony Wawina-Bokalanga, .et al. , EBioMedicine, 2024, Dec:110:105488 PMID: 39615460
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antifungal agent
Propylparaben is an antifungal agent.- Jingyeong Shin, .et al. , Chemical Engineering Journal, 2023, December
- Ethylparaben is the ethyl ester of p-hydroxybenzoic acid, used as an antifungal preservative and food additive. It is a standardized chemical allergen.
- Jingyeong Shin, .et al. , Chemical Engineering Journal, 2023, December
- VX-787 is a novel inhibitor of influenza virus replication that blocks the PB2 cap-snatching activity of the influenza viral polymerase complex.
- Jiri Gregor, .et al. , Molecules, 2021, Feb; 26(4): 1007 PMID: 33673017
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HIV-1 protease inhibitor
Nelfinavir is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection.- Joanna Ireland, .et al. , Front Microbiol, 2024, Mar 20:15:1385775 PMID: 38572241
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Yang PM, .et al. , Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
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IMPDH inhibitor
AVN-944 (also known as VX-944) serves as an effective oral inhibitor, specifically targeting and inhibiting IMPDH (inosine monophosphate dehydrogenase). This enzyme plays a crucial role as a rate-limiting factor in the synthesis of guanine nucleotides from scratch. Additionally, AVN-944 acts against the synthesis of RNA in arenaviruses, effectively preventing arenavirus infections. Demonstrating a wide spectrum of anti-cancer properties, AVN-944 is utilized in research related to multiple myeloma (MM) and acute myeloid leukemia (AML).
- Kevin Chiem, .et al. , Microbiol Spectr, 2023, Aug 17;11(4):e0474522 PMID: PMC10434227
- Desarey Morales Vasquez, .et al. , Viruses, 2020, Sep; 12(9): 1041 PMID: 32961956
- Park JG, .et al. , J Virol, 2020, Mar 17;94(7) PMID: 31941776
- Dunham EC, .et al. , Antiviral Res, 2018, Sep;157:140-150 PMID: 30031760
- Aciclovir is an antiviral agent primarily used for the treatment of herpes simplex virus infections, as well as in the treatment of varicella zoster (chickenpox) and herpes zoster (shingles). It was seen as the start of a new era in antiviral therapy, as it is extremely selective and low in cytotoxicity.
- Kyra-Elisa Maria Redeker, .et al. , Biomolecules, 2022, Nov 9;12(11):1664 PMID: 36359014
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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HIV integrase inhibitor
S/GSK1349572 is a potent next generation HIV integrase inhibitor and demonstrates a superior resistance profile substantiated with 60 integrase mutant molecular clones.- Lea El Khoury, .et al. , PeerJ Preprints, 2019, 7:e27833v1
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HIV integrase inhibitor
Elvitegravir (GS-9137) is a potent inhibitor of the strand-transfer step of integration mediated by human immunodeficiency virus type 1 (HIV-1) integrase.- Lea El Khoury, .et al. , PeerJ Preprints, 2019, 7:e27833v1
- El Khoury L, .et al. , Biochem Biophys Res Commun, 2017, Jul 1;488(3):433-438 PMID: 28478035
- Colistin is a cyclic cationic decapeptide linked to a fatty acid side chain, it belongs to a group of similarly structured bacterial antimicrobial peptides.
- Matteo Bassetti, .et al. , Antimicrob Resist Infect Control, 2024, Aug 26;13(1):91 PMID: 39183351
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protein synthesis inhibitor
Retapamulin is an antibacterial agent, specifically a protein synthesis inhibitor- Merianne Mohamad, .et al. , Nucleic Acids Res, 2022, Feb 28;50(4):2128-2142 PMID: 35137182
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HIV-1 integrase Inhibitor
Bictegravir, also known as GS-9883, is a potent, unboosted, once-Daily HIV-1 Integrase Strand Transfer Inhibitor (INSTI) (IC50 - 1.6 nM) with improved pharmacokinetics and in vitro resistance profile.- Michal S Barski, .et al. , Nat Commun, 2021, Aug 17;12(1):4996 PMID: 34404793
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HIV-1 integrase inhibitor
Raltegravir (MK-0518) targets integrase, an HIV enzyme that integrates the viral genetic material into human chromosomes, a critical step in the pathogenesis of HIV.- Min Li, .et al. , J Infect Dis, 2025, Jul 16:jiaf373
- Joanna Ireland, .et al. , Front Microbiol, 2024, Mar 20:15:1385775 PMID: 38572241
- Michal S Barski, .et al. , Nat Commun, 2021, Aug 17;12(1):4996 PMID: 34404793
- Lea El Khoury, .et al. , PeerJ Preprints, 2019, 7:e27833v1
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HIV-1 attachment inhibitor
BMS-663068 is an HIV-1 attachment inhibitor in development for the treatment of HIV-1 infection.- Min Li, .et al. , J Infect Dis, 2025, Jul 16:jiaf373
- Min Li, .et al. , Nat Commun, 2020, 11: 4051 PMID: 32792548
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HIV-1 maturation inhibitor
Bevirimat (MPC-4326, PA-457, YK-FH312) is a first-in-class HIV-1 maturation inhibitor that demonstrates high potency in cell culture and has shown clinical efficacy in HIV-1-infected patients.- Mingzhang Wang, .et al. , Nat Commun, 2017, 8: 1779 PMID: 29176596
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Glycopeptide Antibiotic
Bleomycin is a glycopeptide antibiotic produced by the bacterium Streptomyces verticillus. It acts by induction of DNA strand breaks.- Ou QX, .et al. , Bioelectrochemistry, 2017, Jun;115:47-55 PMID: 28063751
- PA-824 is an experimental anti-tuberculosis drug.
- Pablo Rodríguez-Fernández, .et al. , ACS Infect Dis, 2024, Jan 12;10(1):170-183 PMID: 38085851
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Thanh Quang Nguyen, .et al. , Antimicrob Agents Chemother, 2022, Dec 20;66(12):e0044822 PMID: 36321819
- Wang X, .et al. , Cell Chem Biol, 2019, Nov 7. pii: S2451-9456(19)30355-1 PMID: 31711854
- Alexandre López-Gavín, .et al. , Int J Antimicrob Agents., 2015, Nov;46(5):582-5 PMID: 26421981
- Imipenem is an intravenous betalactam antibiotic discovered by Merck scientists Burton Christensen, William Leanza, and Kenneth Wildonger in 1980.
- Rachel F. Rollo, .et al. , Microbiol Spectr, 2023, Jul-Aug; 11(4) PMID: 37289062
- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
- Hongwei Liu, .et al. , New Phytol, 2020, Oct 31 PMID: 33131088
- Pholwat S, .et al. , PLoS One, 2019, May 10;14(5):e0216747 PMID: 31075137
- Meikle V, .et al. , Antimicrob Agents Chemother, 2018, Nov 12. pii: AAC.01846-18 PMID: 30420480
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Antibiotic
Delamanid is a new antituberculosis drug that inhibits mycolic acid synthesis and has shown potent in vitro and in vivo activity against drug-resistant strains of Mycobacterium tuberculosis.- Seungmo Kim, .et al. , Tuberculosis, 2025, 152: 102630
- Thanh Quang Nguyen, .et al. , Antimicrob Agents Chemother, 2022, Dec 20;66(12):e0044822 PMID: 36321819
- Meikle V, .et al. , Antimicrob Agents Chemother, 2018, Nov 12. pii: AAC.01846-18 PMID: 30420480
- World Health Organization, .et al. , World Health Organization, 2018, WHO/CDS/TB/2018.24
- Sitafloxacin is a new-generation, broad-spectrum oral fluoroquinolone that is very active against many Gram-positive, Gram-negative and anaerobic clinical isolates, including strains resistant to other fluoroquinolones, was recently approved in Japan for the treatment of respiratory and urinary tract infections. Sitafloxacin is active against methicillin-resistant staphylococci, Streptococcus pneumoniae and other streptococci with reduced susceptibility to levofloxacin and other quinolones and enterococci.
- Seyedeh Bita Mousavinafchi, .et al. , Food Sci Nutr, 2022, Nov 21;11(2):1142-1153 PMID: 36789060
- Aztreonam is a synthetic monocyclic beta-lactam antibiotic (a monobactam), with the nucleus based on a simpler monobactam isolated from Chromobacterium violaceum.
- Sreevalli Sharma, .et al. , ACS Infect Dis, 2021, Nov 12;7(11):3009-3024 PMID: 34699190
- Pholwat S, .et al. , PLoS One, 2019, May 10;14(5):e0216747 PMID: 31075137
- Robert Bucki, .et al. , Infect Drug Resist, 2018, 11: 77-86 PMID: 29391814
- Sodium Tauroursodeoxycholate (TUDC) is a water soluble bile salt, used for the treatment of gallstones and liver cirrhosis.
- Stella Liong, .et al. , Mol Cell Endocrinol, 2016, Apr 15;425:11-25 PMID: 26902174
- SQ109 is an orally active, small molecule antibiotic for treatment of pulmonary T(tuberculosis).
- Thanh Quang Nguyen, .et al. , Antimicrob Agents Chemother, 2022, Dec 20;66(12):e0044822 PMID: 36321819
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DprE inhibitor
Macozinone (PBTZ169) is a bactericidal benzothiazinone and a potent DprE1 (decaprenylphosphoryl-β-d-ribose 2'-oxidase) inhibitor.
- Thanh Quang Nguyen, .et al. , Antimicrob Agents Chemother, 2022, Dec 20;66(12):e0044822 PMID: 36321819
- Tigecycline is bacteriostatic and is a protein synthesis inhibitor by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation.
- Thanh Quang Nguyen, .et al. , Microbiol Spectr, 2023, Jun 15;11(3):e0063123 PMID: 37158736
- Zewen Wen, .et al. , J Antibiot (Tokyo), 2022, Sep;75(9):498-508 PMID: 35896611
- Xiaoming Liu, .et al. , J Antibiot (Tokyo), 2022, Aug;75(8):463-471 PMID: 35760902
- Sato T, .et al. , Microb Drug Resist, 2018, Jul/Aug;24(6):860-867 PMID: 29232167
- Dinah B. Aziz, .et al. , Front Microbiol, 2018, May 11 PMID: 29867841
- Toyotaka Sato, .et al. , Antimicrob Agents Chemother, 2017, Feb; 61(2): e01654-16 PMID: 27855067
- Fusidate Sodium is a sodium salt form of fusidic acid, a bacteriostatic antibiotic derived from the fungus Fusidium coccineum and used as a topical medication to treat skin infections.
- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
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antibiotic
Cefoxitin Sodium is a semisynthetic cephamycin antibiotic resistant to beta-lactamase. It is derived from Cephamycin C and is highly resistance to β-lactamase inactivation.- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
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Topoisomerase IV inhibitor
Ciprofloxacin Hydrochloride is a broad-spectrum antimicrobial carboxyfluoroquinoline, interfering with the bacterial DNA gyrase, inhibiting the DNA synthesis, and preventing bacterial cell growth.- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
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broad-spectrum antibiotic
Tobramycin Sulfate is a broad-spectrum antibiotic. It is effective against gram-negative bacteria, and especially potent against the Pseudomonas species.- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
- Ampicillin Trihydrate is a beta-lactam antibiotic, which inhibits bacterial cell-wall synthesis (peptidoglycan cross-linking) by inactivating transpeptidases on the inner surface of the bacterial cell membrane.
- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
- Cefazolin Sodium is a semisynthetic cephalosporin analog with broad-spectrum antibiotic action due to inhibition of bacterial cell wall synthesis. It attains high serum levels and is excreted quickly via the urine.
- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
- Clindamycin inhibits protein synthesis by acting on the 50S ribosomal, used for the treatment of bacterial infections.
- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
- Cloxacillin is a semisynthetic antibiotic in the same class as penicillin. Cloxacillin is used against staphylococci that produce beta-lactamase, due to its large R chain, which does not allow the beta-lactamases to bind.
- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
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DDX3 inhibitor
DDX3-IN-1 (Compound 16f) is a DEAD-box polypeptide 3 (DDX3) inhibitor with CC50s of 50 and 36 μM for HIV and HCV, respectively. Antiviral activity.- Wensheng Chen, .et al. , JCI Insight, 2023, Apr 10;8(7):e167566 PMID: 36821384
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midazopyridine amide compound
Q203 (IAP6) is a midazopyridine amide compound. Q203 is active against Mycobacterium tuberculosis H37Rv with an MIC50 of 2.7 nM in culture broth medium. - Moxidectin is an anthelmintic drug which kills parasitic worms (helminths), and is used for the prevention and control of heartworm and intestinal worms.
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non-ionic emulsifying agent
Polyoxyethylene stearate (POES) is a non-ionic emulsifying agent. -
DprE1 inhibitor
DprE1-IN-2 (compound 18) is a potent DprE1 inhibitor with an IC50 of 28 nM. DprE1-IN-2 has antituberculosis effect. -
squalene synthetase inhibitor
YM-53601 free base is a squalene synthetase inhibitor which suppresses lipogenic biosynthesis and lipid secretion in rodents.

