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New treatment for drug-resistant bacterial infection: Taigexyn® (Nemonoxacin)


Taigexyn®

Taigexyn® (Nemonoxacin) is a novel broad spectrum antibiotic for treatment of bacterial infections. It belongs to a new class of antibiotics known as non-fluorinated quinolone. Taigexyn® was discovered by screening against antibiotic-resistant bacteria and thus has intrinsic activity against the resistant infection which is an increasingly severe problem worldwide. Taigexyn® differentiates itself from the current antibiotics on the market by the following characteristics:

Broad spectrum activities against Gram-positive, Gram-negative, anaerobic, and atypical pathogens.

Superior activity against drug resistant pathogens – especially MRSA and Quinolone-resistant MRSA.

Reduced propensity for resistance development – requires mutations in three different bacterial genes.

Excellent pharmacokinetic profile suitable for once-a-day oral or iv dosing.


Clinical Development

Nemonoxacin’s safety and efficacy had already been demonstrated in clinical studies performed in multinational and multicenter trials.

Completed Phase I~III CAP study for the oral formulation in China and Taiwan.

Taigexyn® capsule was approved and launched in Taiwan and mainland China. It is the first Class 1 new drug developed by a Taiwanese company to receive market approval in mainland China. It is also the first new drug approval after the NMPA announced the requirement of self-inspection of drug clinical trial data in July 2015.

For the IV formulation, successfully completed Phase III clinical trials in Taiwan and China. In May 2017, filed DNA for IV formulation in China and expect to receive marketing approval soon; In Taiwan, Phase III endpoint was successfully achieved, currently prepare for NDA filing.

Completed Phase I and Phase II studies in Community Acquired Pneumonia (CAP) and Diabetic Foot Infection (DFI) under US IND.

Received QIDP (Qualified Infectious Disease Product) and Fast Track status for CAP and ABSSSI (acute bacterial skin and skin structure infections) from US FDA.

Licensed to Zhejiang Medicine in China and R-Pharm in Russia, Productos Científicos in Latin America.


Intellectual Property

Nemonoxacin is protected globally by a portfolio of patents that cover composition of matter, use and manufacturing process up to 2029.


Awards and Grants

Received grants from the Taiwan Ministry of Economic Affairs for preclinical, Phase 1, 2, and 3 clinical development.

Out-licensed to Zhejiang Medicine in mainland China in 2012.

Awarded the National Innovation Award from Taiwan's Institute for Biotechnology and Medicine Industry and the Taipei Biotech Award for Technology Transfer in 2013.

Out-licensed to R-Pharm for Russia, Commonwealth Independent States and Turkey markets in 2014.

Awarded the Innovation of the Year from the Taiwan Bio Industry Organization and Golden Innovation Award from TFDA & Ministry of Economic Affair in 2015.

Out-licensed to Productos Científicos for Latin American markets in 2016.


Presentations


2017 ECCMID

In vitro Activity of Nemonoxacin Against Streptococcus pnuemoniae and Haemophilus influenzae– Poster EVO440 R.S. KOZLOV, A.V. DEKHNICH, M.V. SUKHORUKOVA, M.V. EDELSTEIN, A.V. CHERNAVIN, M.Y. SAMSONOV


2015 ATS

Efficacy and Safety of Oral Nemonoxacin in Treatment of Community-Acquired Pneumonia: Subgroup Analysis Results in Taiwanese Patients in a Randomized, Double-Blind, Multi-Center, Phase III Comparative Study with Levofloxacin – Poster 63714 S. L. CHENG, R. G. WU, Z. HSU, C. H. R. KING, P. HUANG, L. W. CHANG, J. YUAN, J. CHANG, P. T. HUANG, C. E. TSAI


2014 ICAAC

Meeting the Threat of Antibiotic Resistance: In Vitro Activity, Clinical Efficacy and Safety of Nemonoxacin, a Novel Non-Fluorinated Quinolone with QIDP Status – Poster L-1748b C. E. TSAI, Z. HSU, C. H. R. KING, P. HUANG, L. W. CHANG, J. YUAN, J. CHANG, P. T. HUANG, M. C. HSU

Efficacy and Safety of Oral Nemonoxacin in Treatment of Community-Acquired Pneumonia: Results from a Randomized, Double-Blind, Multiple-Center, Phase III Comparison Study with Levofloxacin– Poster L-1748c Y. Y. ZHANG, S. L. CHENG, C. E. TSAI, Z. HSU, C. H. R. KING, P. HUANG, L. W. CHANG, J. YUAN, J. CHANG, P. T. HUANG, M. C. HSU


2013 ICAAC

In Vitro Activity of Nemonoxacin, a Novel Quinolone Antibiotic, against Chlamydia pneumonia – Poster E-1182 K. CHOTIKANATIS, S. A. KOHLHOFF, M. R. HAMMERSCHLAG.


2010 ICAAC

Nemonoxacin for Treating Diabetic Foot Infections: An Open-Label, Single-Arm, Multiple-Center Study – Poster L1-344 B. A. LIPSKY, M. GANI, L. ROGERS, J. S. HWANG, D. T. CHUNG, C. Y. TSAI, L. W. CHANG, Y. T. CHANG, C. H. R. KING, M. C. HSU.


2008 ICAAC/IDSA

Comparative Antistaphylococcal activity of Nemonoxacin, a Novel Broad-spectrum Quinolone – Poster C1-189 G. A. PANKUCH, K. KOSOWSKA-SHICK, P. MCGHEE, C. R. KING , P. C. APPELBAUM .

In Vivo Efficacy of Nemonoxacin in a Mouse Protection Model – Poster B-1005 C. H. HSU, L. LIN, R. LEUNK, D. REICHART.

In Vivo Efficacy of Nemonoxacin in a Mouse Pulmonary Infection Model – Poster B-056 C. H. HSU, L. LIN, R. LEUNK, D. REICHART.

Efficacy and Safety of Nemonoxacin versus Levofloxacin for the Treatment of Community-Acquired Pneumonia – Poster L-678 D. J. VAN RENSBURG, R. P. PERNG, L. LIN, H. ZHANG.

In Vitro Resistance Development to Nemonoxacin for Streptococcus pneumoniae – Poster F1-2055 C. R. KING, L. LIN, R. LEUNK.

Fertility and Early Embryonic Developmental Toxicity of Nemonoxacin after Oral Administration to Rats – Poster F1-2056 C. H. HSU, Y. M. CHEN, C. P. CHOW.

Activity of Nemonoxacin, an Investigational C8-methoxy Non-fluorinated Quinolone Against Gram-Positive Cocci Obtained From Canadian Hospitals: CANWARD 2007 – Poster F1-2057 G. G. ZHANEL, M. LAING, M. DECORBY, K. NICHOL, C.H.R. KING, H. ADAM, D. J. HOBAN.

Activity of Nemonoxacin, an Investigational C8-methoxy Non-fluorinated Quinolone, Against Gram-Negative Bacilli Obtained From Canadian Hospitals: CANWARD 2007 – Poster C1-1957 N. LAING, M. DECORBY, K. NICHOL, C.H.R. KING, H. ADAM, D. J. HOBAN, G. G. ZHANEL.

In Vitro Activity of Nemonoxacin (TG-873870), a Novel Non-Fluorinated Quinolone, against Clinical Isolates of Streptococcus pneumoniae in Taiwan – Poster C2-254 P. R. HSUEH, C. KING.

In Vitro Activity of Nemonoxacin against Helicobacter pylori – Poster C2-3931 P.R. HSUEH, J. C. YANG, C. KING.


2008 WPCCID

A Randomized, Double-Blind, Comparative, Multiple-Center Study of Nemonoxacin versus Levofloxacin for the Treatment of Community-Acquired Pneumonia – Poster PS1-069 H. ZHANG, R. P. PERNG, D. J. J. VAN RENSBURG, L. LIN, H. C. TAN, L. W. CHANG.

Mutant Prevention Concentration of Nemonoxacin (TG-873870), a Novel Non-Fluorinated Quinolone, against Staphylococcus aureus – Poster PS1-066 Y. LIU, Z. LI, R. WANG, Z. ZHAO, M. C. HSU.

Comparative Antistaphylococcal activity of Nemonoxacin, a Novel Broad-spectrum Quinolone – Poster PS1-063 G. A. PANKUCH, K. KOSOWSKA-SHICK, C. R. KING , P. C. APPELBAUM.

In Vitro Antibacterial Activity of Nemonoxacin (TG-873870), a New Non-fluorinated Quinolone, Against Gram-Positive Pathogens – Poster PS1-065 T. L. LAUDERDALE, J. F. LAI, Y. R. SHIAU, H. C. CHEN, C. H. R. KING.

In Vitro Activity of Nemonoxacin (TG-873870) against Staphylococcus aureus, Enterococci, and Streptococcus pneumoniae with Various Resistant Phenotypes in Taiwan – Poster PS1-068 P. R. HSUEH, J. J. LU, C. H. R. KING.


2007 ICAAC

In Vitro Metabolism and Interaction of Nemonoxacin (TG-873870) on Human Hepatic CYP3A4 – Poster A-27 C. P. CHOW, C. Y. TSAI, C. F. YEH, S. J. CHEN.

Phototoxicity of Nemonoxacin (TG-873870) in Hairless Mice – Poster A-28 C. P. CHOW, C. SAMBUCO, A. M. HOBERMAN.

Cardiovascular Safety Evaluation of Nemonoxacin (TG-873870) in Dogs and Monkeys – Poster B-823 C. P. CHOW, C. Y. TSAI, Y. M. CHEN.

In Vitro Antibacterial Activity of Nemonoxacin (TG-873870), a New Non-Fluorinated Quinolone, against Clinical Isolates – Poster E-1635 T. L. LAUDERDALE, Y. R. SHIAU, J. F. LAI, H. C. CHEN, C. H. R. KING.


2007 IDSA

Single-Dose Safety, Tolerability, and Pharmacokinetics of Nemonoxacin (TG-873870), a Novel Potent Broad-Spectrum Non-Fluorinated Quinolone, in Healthy Volunteers – Poster 439 L. LIN, K. M. CHIU, T. K. CHUNG.

Multiple-Dose Study to Access the Safety, Tolerability and Pharmacokinetics of Nemonoxacin (TG-873870), a Novel Potent Broad-Spectrum Non-Fluorinated Quinolone, in Healthy Volunteers – Poster 440 H. ZHANG, K. M. CHIU, T. K. CHUNG, H. C. TAN, L. LIN .

Analysis of Antibacterial Response of Nemonoxacin (TG-873870) Against Major Pathogens from Respiratory Tract and Skin Infections – Poster 441 S. J. CHEN, L. LIN, L. W. CHANG.


Selected Publications

Safety and efficacy of oral nemonoxacin versus levofloxacin in treatment of community-acquired pneumonia: A phase 3, multicenter, randomized, double-blind, double-dummy, active-controlled, non-inferiority trial. Yuan J, Mo B, Ma Z, Lv Y, Cheng SL, Yang Y, Tong Z, Wu R, Sun S, Cao Z, Wu J, Zhu D, Chang L, Zhang Y; Investigator Group of the Phase 3 Study on Oral Nemonoxacin. J Microbiol Immunol Infect. 2017 Aug 2. pii: S1684-1182(17)30151-2. doi: 10.1016/j.jmii.2017.07.011. [Epub ahead of print]

In vitro resistance development to nemonoxacin in Streptococcus pneumoniae: A unique profile for a novel nonfluorinated quinolone. Roychoudhury S, Makin K, Twinem T, Leunk R, Hsu MC. Microb Drug Resist. 2016 Oct;22(7):578-584.

Chemical structure and pharmacokinetics of novel quinolone agents represented by avarofloxacin, delafloxacin, finafloxacin, zabofloxacin and nemonoxacin. Kocsis B, Domokos J, Szabo D. Ann Clin Microbiol Antimicrob. 2016 May 23;15(1):34. doi: 10.1186/s12941-016-0150-4. Review.

Effects of probenecid and cimetidine on the pharmacokinetics of nemonoxacin in healthy Chinese volunteers. Zhang YF, Dai XJ, Yang Y, Chen XY, Tang YB, Tsai CY, Chang LW, Chang YT, Zhong DF. Drug Design, Development and Therapy 2016:10 357-370.

A randomized, double-blind, multicenter Phase II study comparing the efficacy and safety of oral nemonoxacin with oral levofloxacin in the treatment of community-acquired pneumonia. Liu Y, Zhang Y, Wu J, Zhu D, Sun S, Zhao L, Wang X, Liu H, Ren Z, Wang C, Xiu Q, Xiao Z, Cao Z, Cui S, Yang H, Liang Y, Chen P, Lv Y, Hu C, Lv X, Liu S, Kuang J, Li J, Wang D, Chang L. J Microbiol Immunol Infect. 2017 Dec;50(6):811-820.

Pharmacokinetics and pharmacodynamics of multiple-dose intravenous nemonoxacin in healthy Chinese volunteers. Wu XJ, Zhang J, Guo BN, Zhang YY, Yu JC, Cao GY, Chen YC, Zhu DM, Ye XY, Wu JF, Shi YG, Chang LW, Chang YT, Tsai CY. Antimicrob Agents Chemother. 2015 Mar;59(3):1446-1454.

The potential role of nemonoxacin for treatment of common infections. Huang CH, Lai CC, Chen YH, Hsueh PR. Expert Opin Pharmacother. 2015 Feb;16(2):263-270.

Effects of an Al(3+)- and Mg(2+)-containing antacid, ferrous sulfate, and calcium carbonate on the absorption of nemonoxacin (TG-873870) in healthy Chinese volunteers. Zhang YF, Dai XJ, Wang T, Chen XY, Liang L, Qiao H, Tsai CY, Chang LW, Huang PT, Hsu CY, Chang YT, Tsai CE, Zhong DF. Acta Pharmacol Sin. 2014 Dec;35(12):1586-1592.

Determination of a novel nonfluorinated quinolone, nemonoxacin, in human feces and its glucuronide conjugate in human urine and feces by high-performance liquid chromatography-triple quadrupole mass spectrometry. He G, Guo B, Yu J, Zhang J, Wu X, Cao G, Shi Y, Tsai CY. Biomed Chromatogr. 2015 May;29(5):739-748.

Antibacterial activities of nemonoxacin against clinical isolates of Staphylococcus aureus: an in vitro comparison with three fluoroquinolones. Li Z, Liu Y, Wang R, Li A. World J Microbiol Biotechnol. 2014 Nov;30(11):2927-2932.

Safety, tolerability, and pharmacokinetics of intravenous nemonoxacin in healthy chinese volunteers. Cao GY, Zhang J, Zhang YY, Guo BN, Yu JC, Wu XJ, Chen YC, Wu JF, Shi YG. Antimicrob Agents Chemother. 2014 Oct;58(10):6116-21.

Review of nemonoxacin with special focus on clinical development. Qin X, Huang H. Drug Des Devel Ther. 2014 Jul 5;8:765-74.

Nemonoxacin (TG-873870) for treatment of community-acquired pneumonia. Lai CC, Lee KY, Lin SW, Chen YH, Kuo HY, Hung CC, Hsueh PR. Expert Rev Anti Infect Ther. 2014 Apr;12(4):401-17.

In vitro activity of nemonoxacin, a novel nonfluorinated quinolone antibiotic, against Chlamydia trachomatis and Chlamydia pneumoniae. Chotikanatis K, Kohlhoff SA, Hammerschlag MR. Antimicrob Agents Chemother. 2014;58(3):1800-1801.

Trends in the susceptibility of methicillin-resistant Staphylococcus aureus to nine antimicrobial agents, including ceftobiprole, nemonoxacin, and tyrothricin: results from the Tigecycline In Vitro Surveillance in Taiwan (TIST) study, 2006-2010. Chen YH, Liu CY, Ko WC, Liao CH, Lu PL, Huang CH, Lu CT, Chuang YC, Tsao SM, Chen YS, Liu YC, Chen WY, Jang TN, Lin HC, Chen CM, Shi ZY, Pan SC, Yang JL, Kung HC, Liu CE, Cheng YJ, Liu JW, Sun W, Wang LS, Yu KW, Chiang PC, Lee MH, Lee CM, Hsu GJ, Hsueh PR. Eur J Clin Microbiol Infect Dis. 2014 Feb;33(2):233-239.

Pharmacokinetics and Pharmacodynamics of Nemonoxacin against Streptococcus pneumoniae in an In Vitro Infection Model. Liang W, Chen YC, Cao YR, Liu XF, Huang J, Hu JL, Zhao M, Guo QL, Zhang SJ, Wu XJ, Zhu DM, Zhang YY, Zhang J. Antimicrob Agents Chemother. 2013 Jul;57(7):2942-7.

Safety and clinical pharmacokinetics of nemonoxacin, a novel non-fluorinated quinolone, in healthy chinese volunteers following single and multiple oral doses. Guo B, Wu X, Zhang Y, Shi Y, Yu J, Cao G, Zhang J. Clin. Drug Invest. 2012 Jul 1;32(7):475-486.

Characterizations of Clinical Isolates of Clostridium difficile by Toxin Genotypes and by Susceptibility to 12 Antimicrobial Agents, Including Fidaxomicin (OPT-80) and Rifaximin: A Multicenter Study in Taiwan. Liao CH, Ko WC, Lu JJ, Hsueh PR. Antimicrob Agents Chemother. 2012 Jul;56(7):3943-3949.

A liquid chromatography-tandem mass spectrometry assay for the determination of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, in human plasma and urine and its application to a single-dose pharmacokinetic study in healthy Chinese volunteers. Guo B, Zhang J, Yu J, Wu X, Shi Y, Tsai CY. Biomed Chromatogr. 2012 Nov;26(11):1333-1140.

Multicenter Study In Taiwan of the In Vitro Activities of Nemonoxacin, Tigecycline, Doripenem, and Other Antimicrobial Agents against Clinical Isolates of Various Nocardia Species. Lai CC, Liu WL, Ko WC, Chen YH, Tan HR, Huang YT, Hsueh PR. Antimicrob Agents Chemother. 2011 May; 55(5):2084-2091.

In vitro susceptibilities of clinical isolates of ertapenem-non-susceptible Enterobacteriaceae to nemonoxacin, tigecycline, fosfomycin and other antimicrobial agents. Hsu MS, Liao CH, Liu CY, Yang CJ, Huang YT, Hsueh PR. Int J Antimicrob Agents. 2011 Mar;37(3):276-278.

Antimicrobial Susceptibilities and Molecular Epidemiology of Clinical Isolates of Clostridium difficile in Taiwan. Lin YC, Huang YT, Tsai PJ, Lee TF, Lee NY, Liao CH, Lin SY, Ko WC, Hsueh PR. Antimicrob Agents Chemother. 2011 Apr; 55(4);1701-1705.

In vivo antibacterial activity of nemonoxacin, a novel non-fluorinated quinolone. Li CR, Li Y, Li GQ, Yang XY, Zhang WX, Lou RH, Liu JF, Yuan M, Huang P, Cen S, Yu LY, Zhao LX, Jiang JD, You XF. J Antimicrob Chemother. 2010 Nov;65(11):2411-2415.

Efficacy and safety of nemonoxacin versus levofloxacin for community-acquired pneumonia. Dirkie J. J. van Rensburg, Reury-Perng Perng, Ismail H. Mitha, Andrè J.Bester, Joseph Kasumba, Ren-Guang Wu, Ming-Lin Ho, Li-Wen Chang, David T. Chung, Yu-Ting Chang,Chi-Hsin R. King, and Ming-Chu Hsu. Antimicrob Agents Chemother. 2010 Oct;54(10):4098-4106.

In vitro activity of nemonoxacin, tigecycline, and other antimicrobial agents against Helicobacter pylori isolates in Taiwan, 1998-2007. Yang JC, Lee PI, Hsueh PR. Eur J Clin Microbiol Infect Dis. 2010 Nov;29(11):1369-1375.

Comparative in vitro activities of nemonoxacin, (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates. Tsai-Ling Lauderdale, Yih-Ru Shiau, Jui-Fen Lai, Hua-Chien Chen, and Chi-Hsin R. King. Antimicrob Agents Chemother. 2010 Mar; 54(3):1338-42.

Multiple-Dose Safety, Tolerability, and Pharmacokinetics of Oral Nemonoxacin (TG-873870) in Healthy Volunteers. David T. Chung, Cheng-Yuan Tsai, Shu-Jen Chen, Li-Wen Chang, Chi-Hsin R. King, Ching-Hung Hsu, Kit-Mui Chiu, Hao-Chen Tan, Yu-Ting Chang, and Ming-Chu Hsu. Antimicrob Agents Chemother. 2010 Jan; 45(1):411-417.

Dose-Escalation Study of the Safety, Tolerability, and Pharmacokinetics of Nemonoxacin (TG-873870), a Novel Potent Broad-Spectrum Non-Fluorinated Quinolone, in Healthy Volunteers. Luke Lin, Li-Wen Chang, Cheng-Yuan Tsai, Ching-Hung Hsu, David T. Chung, William S. Aronstein, Funmi Ajayi, Barbara Kuzmak, and Robert A. Lyon. Antimicrob Agents Chemother. 2010 Jan;45(1):405-410.

In vitro activity of nemonoxacin (TG-873870), a novel non-fluorinated quinolone, against clinical isolates of Staphylococcus aureus, Enterococci, and Streptococcus pneumoniae with various resistant phenotypes in Taiwan. Yeh-Hsu Chen, Chia-Ying Liu, Jang-Jih Lu, Chi-Hsin R. King, and Po-Ren Hsueh. J Antimicrob Chemother. 2009 Dec;64(6):1226-1229.

Comparative in vitro activities of the new quinolone nemonoxacin (TG-873870), gemifloxacin and other quinolones against clinical isolates of Mycobacterium tuberculosis. Che-Kim Tan, Chih-Cheng Lai, Chun-Hsing Liao, Chien-Hong Chou, Hsiao-Leng Hsu, Yu-Tsung Huang and Po-Ren Hsueh. J Antimicrob Chemother. 2009 Aug;64(2):428-429.

Comparative in vitro activities of nemonoxacin, doripenem, tigecycline and 16 other antimicrobials against Nocardia brasiliensis, Nocardia asteroides and unusual Nocardia species. Chih-Cheng Lai, Che-Kim Tan, Sheng Hsiang Lin, Chun-Hsing Liao, Chien-Hong Chou, Hsiao-Leng Hsu, Yu-Tsung Huang, and Po-Ren Hsueh. J Antimicrob Chemother. 2009 Jul;64(1):73-78.

Nemonoxacin. Arjona, A, Castaner, R, Bolos, J. Drugs of the Future. 2009 Mar; 34(3): 196-203.