Multiple-Ascending-Dose Phase 1 Clinical Study of the Safety, Tolerability, and Pharmacokinetics of CRS3123, a Narrow-Spectrum Agent with Minimal Disruption of Normal Gut Microbiota

CRS3123 is a novel small molecule that potently inhibits methionyl-tRNA synthetase of Clostridioides difficile , inhibiting C. difficile toxin production and spore formation. CRS3123 has been evaluated in a multiple-ascending-dose placebo-controlled phase 1 trial. CRS3123 is a novel small molecule t...

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Published inAntimicrobial agents and chemotherapy Vol. 64; no. 1
Main Authors Lomeli, Barbara K., Galbraith, Hal, Schettler, Jared, Saviolakis, George A., El-Amin, Wael, Osborn, Blaire, Ravel, Jacques, Hazleton, Keith, Lozupone, Catherine A., Evans, Ronald J., Bell, Stacie J., Ochsner, Urs A., Jarvis, Thale C., Baqar, Shahida, Janjic, Nebojsa
Format Journal Article
LanguageEnglish
Published United States American Society for Microbiology 20.12.2019
Subjects
Online AccessGet full text
ISSN0066-4804
1098-6596
1070-6283
1098-6596
DOI10.1128/AAC.01395-19

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Abstract CRS3123 is a novel small molecule that potently inhibits methionyl-tRNA synthetase of Clostridioides difficile , inhibiting C. difficile toxin production and spore formation. CRS3123 has been evaluated in a multiple-ascending-dose placebo-controlled phase 1 trial. CRS3123 is a novel small molecule that potently inhibits methionyl-tRNA synthetase of Clostridioides difficile , inhibiting C. difficile toxin production and spore formation. CRS3123 has been evaluated in a multiple-ascending-dose placebo-controlled phase 1 trial. Thirty healthy subjects, ages 18 to 45 years, were randomized into three cohorts of 10 subjects each, receiving either 200, 400, or 600 mg of CRS3123 (8 subjects per cohort) or placebo (2 subjects per cohort) by oral administration twice daily for 10 days. CRS3123 was generally safe and well tolerated, with no serious adverse events (SAEs) or severe treatment-emergent adverse events (TEAEs) reported. All subjects completed their assigned treatment and follow-up visits, and there were no trends in systemic, vital sign, or laboratory TEAEs. There were no QTcF interval changes or any clinically significant changes in other electrocardiogram (ECG) intervals or morphology. CRS3123 showed limited but detectable systemic uptake; although absorption increased with increasing dose, the increase was less than dose proportional. Importantly, the bulk of the oral dose was not absorbed, and fecal concentrations were substantially above the MIC 90 value of 1 μg/ml at all dosages tested. Subjects receiving either of the two lower doses of CRS3123 exhibited minimal disruption of normal gut microbiota after 10 days of twice-daily dosing. CRS3123 was inactive against important commensal anaerobes, including Bacteroides , bifidobacteria, and commensal clostridia. Microbiome data showed favorable differentiation compared to other CDI therapeutics. These results support further development of CRS3123 as an oral agent for the treatment of CDI. (This study has been registered at Clinicaltrials.gov under identifier NCT02106338.)
AbstractList CRS3123 is a novel small molecule that potently inhibits methionyl-tRNA synthetase of , inhibiting toxin production and spore formation. CRS3123 has been evaluated in a multiple-ascending-dose placebo-controlled phase 1 trial. Thirty healthy subjects, ages 18 to 45 years, were randomized into three cohorts of 10 subjects each, receiving either 200, 400, or 600 mg of CRS3123 (8 subjects per cohort) or placebo (2 subjects per cohort) by oral administration twice daily for 10 days. CRS3123 was generally safe and well tolerated, with no serious adverse events (SAEs) or severe treatment-emergent adverse events (TEAEs) reported. All subjects completed their assigned treatment and follow-up visits, and there were no trends in systemic, vital sign, or laboratory TEAEs. There were no QTcF interval changes or any clinically significant changes in other electrocardiogram (ECG) intervals or morphology. CRS3123 showed limited but detectable systemic uptake; although absorption increased with increasing dose, the increase was less than dose proportional. Importantly, the bulk of the oral dose was not absorbed, and fecal concentrations were substantially above the MIC value of 1 μg/ml at all dosages tested. Subjects receiving either of the two lower doses of CRS3123 exhibited minimal disruption of normal gut microbiota after 10 days of twice-daily dosing. CRS3123 was inactive against important commensal anaerobes, including , bifidobacteria, and commensal clostridia. Microbiome data showed favorable differentiation compared to other CDI therapeutics. These results support further development of CRS3123 as an oral agent for the treatment of CDI. (This study has been registered at Clinicaltrials.gov under identifier NCT02106338.).
CRS3123 is a novel small molecule that potently inhibits methionyl-tRNA synthetase of Clostridioides difficile, inhibiting C. difficile toxin production and spore formation. CRS3123 has been evaluated in a multiple-ascending-dose placebo-controlled phase 1 trial. Thirty healthy subjects, ages 18 to 45 years, were randomized into three cohorts of 10 subjects each, receiving either 200, 400, or 600 mg of CRS3123 (8 subjects per cohort) or placebo (2 subjects per cohort) by oral administration twice daily for 10 days. CRS3123 was generally safe and well tolerated, with no serious adverse events (SAEs) or severe treatment-emergent adverse events (TEAEs) reported. All subjects completed their assigned treatment and follow-up visits, and there were no trends in systemic, vital sign, or laboratory TEAEs. There were no QTcF interval changes or any clinically significant changes in other electrocardiogram (ECG) intervals or morphology. CRS3123 showed limited but detectable systemic uptake; although absorption increased with increasing dose, the increase was less than dose proportional. Importantly, the bulk of the oral dose was not absorbed, and fecal concentrations were substantially above the MIC90 value of 1 μg/ml at all dosages tested. Subjects receiving either of the two lower doses of CRS3123 exhibited minimal disruption of normal gut microbiota after 10 days of twice-daily dosing. CRS3123 was inactive against important commensal anaerobes, including Bacteroides, bifidobacteria, and commensal clostridia. Microbiome data showed favorable differentiation compared to other CDI therapeutics. These results support further development of CRS3123 as an oral agent for the treatment of CDI. (This study has been registered at Clinicaltrials.gov under identifier NCT02106338.).CRS3123 is a novel small molecule that potently inhibits methionyl-tRNA synthetase of Clostridioides difficile, inhibiting C. difficile toxin production and spore formation. CRS3123 has been evaluated in a multiple-ascending-dose placebo-controlled phase 1 trial. Thirty healthy subjects, ages 18 to 45 years, were randomized into three cohorts of 10 subjects each, receiving either 200, 400, or 600 mg of CRS3123 (8 subjects per cohort) or placebo (2 subjects per cohort) by oral administration twice daily for 10 days. CRS3123 was generally safe and well tolerated, with no serious adverse events (SAEs) or severe treatment-emergent adverse events (TEAEs) reported. All subjects completed their assigned treatment and follow-up visits, and there were no trends in systemic, vital sign, or laboratory TEAEs. There were no QTcF interval changes or any clinically significant changes in other electrocardiogram (ECG) intervals or morphology. CRS3123 showed limited but detectable systemic uptake; although absorption increased with increasing dose, the increase was less than dose proportional. Importantly, the bulk of the oral dose was not absorbed, and fecal concentrations were substantially above the MIC90 value of 1 μg/ml at all dosages tested. Subjects receiving either of the two lower doses of CRS3123 exhibited minimal disruption of normal gut microbiota after 10 days of twice-daily dosing. CRS3123 was inactive against important commensal anaerobes, including Bacteroides, bifidobacteria, and commensal clostridia. Microbiome data showed favorable differentiation compared to other CDI therapeutics. These results support further development of CRS3123 as an oral agent for the treatment of CDI. (This study has been registered at Clinicaltrials.gov under identifier NCT02106338.).
CRS3123 is a novel small molecule that potently inhibits methionyl-tRNA synthetase of Clostridioides difficile , inhibiting C. difficile toxin production and spore formation. CRS3123 has been evaluated in a multiple-ascending-dose placebo-controlled phase 1 trial. CRS3123 is a novel small molecule that potently inhibits methionyl-tRNA synthetase of Clostridioides difficile , inhibiting C. difficile toxin production and spore formation. CRS3123 has been evaluated in a multiple-ascending-dose placebo-controlled phase 1 trial. Thirty healthy subjects, ages 18 to 45 years, were randomized into three cohorts of 10 subjects each, receiving either 200, 400, or 600 mg of CRS3123 (8 subjects per cohort) or placebo (2 subjects per cohort) by oral administration twice daily for 10 days. CRS3123 was generally safe and well tolerated, with no serious adverse events (SAEs) or severe treatment-emergent adverse events (TEAEs) reported. All subjects completed their assigned treatment and follow-up visits, and there were no trends in systemic, vital sign, or laboratory TEAEs. There were no QTcF interval changes or any clinically significant changes in other electrocardiogram (ECG) intervals or morphology. CRS3123 showed limited but detectable systemic uptake; although absorption increased with increasing dose, the increase was less than dose proportional. Importantly, the bulk of the oral dose was not absorbed, and fecal concentrations were substantially above the MIC 90 value of 1 μg/ml at all dosages tested. Subjects receiving either of the two lower doses of CRS3123 exhibited minimal disruption of normal gut microbiota after 10 days of twice-daily dosing. CRS3123 was inactive against important commensal anaerobes, including Bacteroides , bifidobacteria, and commensal clostridia. Microbiome data showed favorable differentiation compared to other CDI therapeutics. These results support further development of CRS3123 as an oral agent for the treatment of CDI. (This study has been registered at Clinicaltrials.gov under identifier NCT02106338.)
CRS3123 is a novel small molecule that potently inhibits methionyl-tRNA synthetase of Clostridioides difficile, inhibiting C. difficile toxin production and spore formation. CRS3123 has been evaluated in a multiple-ascending-dose placebo-controlled phase 1 trial. CRS3123 is a novel small molecule that potently inhibits methionyl-tRNA synthetase of Clostridioides difficile, inhibiting C. difficile toxin production and spore formation. CRS3123 has been evaluated in a multiple-ascending-dose placebo-controlled phase 1 trial. Thirty healthy subjects, ages 18 to 45 years, were randomized into three cohorts of 10 subjects each, receiving either 200, 400, or 600 mg of CRS3123 (8 subjects per cohort) or placebo (2 subjects per cohort) by oral administration twice daily for 10 days. CRS3123 was generally safe and well tolerated, with no serious adverse events (SAEs) or severe treatment-emergent adverse events (TEAEs) reported. All subjects completed their assigned treatment and follow-up visits, and there were no trends in systemic, vital sign, or laboratory TEAEs. There were no QTcF interval changes or any clinically significant changes in other electrocardiogram (ECG) intervals or morphology. CRS3123 showed limited but detectable systemic uptake; although absorption increased with increasing dose, the increase was less than dose proportional. Importantly, the bulk of the oral dose was not absorbed, and fecal concentrations were substantially above the MIC90 value of 1 μg/ml at all dosages tested. Subjects receiving either of the two lower doses of CRS3123 exhibited minimal disruption of normal gut microbiota after 10 days of twice-daily dosing. CRS3123 was inactive against important commensal anaerobes, including Bacteroides, bifidobacteria, and commensal clostridia. Microbiome data showed favorable differentiation compared to other CDI therapeutics. These results support further development of CRS3123 as an oral agent for the treatment of CDI. (This study has been registered at Clinicaltrials.gov under identifier NCT02106338.)
CRS3123 is a novel small molecule that potently inhibits methionyl-tRNA synthetase of Clostridioides difficile, inhibiting C. difficile toxin production and spore formation. CRS3123 has been evaluated in a multiple-ascending-dose placebo-controlled phase 1 trial. Thirty healthy subjects, ages 18 to 45 years, were randomized into three cohorts of 10 subjects each, receiving either 200, 400, or 600 mg of CRS3123 (8 subjects per cohort) or placebo (2 subjects per cohort) by oral administration twice daily for 10 days. CRS3123 was generally safe and well tolerated, with no serious adverse events (SAEs) or severe treatment-emergent adverse events (TEAEs) reported. All subjects completed their assigned treatment and follow-up visits, and there were no trends in systemic, vital sign, or laboratory TEAEs. There were no QTcF interval changes or any clinically significant changes in other electrocardiogram (ECG) intervals or morphology. CRS3123 showed limited but detectable systemic uptake; although absorption increased with increasing dose, the increase was less than dose proportional. Importantly, the bulk of the oral dose was not absorbed, and fecal concentrations were substantially above the MIC90 value of 1 μg/ml at all dosages tested. Subjects receiving either of the two lower doses of CRS3123 exhibited minimal disruption of normal gut microbiota after 10 days of twice-daily dosing. CRS3123 was inactive against important commensal anaerobes, including Bacteroides, bifidobacteria, and commensal clostridia. Microbiome data showed favorable differentiation compared to other CDI therapeutics. These results support further development of CRS3123 as an oral agent for the treatment of CDI. (This study has been registered at Clinicaltrials.gov under identifier NCT02106338.)
Author Lomeli, Barbara K.
Schettler, Jared
Evans, Ronald J.
Osborn, Blaire
Lozupone, Catherine A.
Galbraith, Hal
Bell, Stacie J.
Ravel, Jacques
Jarvis, Thale C.
El-Amin, Wael
Baqar, Shahida
Janjic, Nebojsa
Saviolakis, George A.
Hazleton, Keith
Ochsner, Urs A.
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Cites_doi 10.1080/17512433.2017.1362978
10.1086/430315
10.1016/j.cmi.2014.08.017
10.1093/cid/cix1085
10.1186/2049-2618-2-6
10.1111/j.1365-2362.2012.02659.x
10.1056/NEJMoa1602615
10.1093/jac/dkp041
10.1093/bioinformatics/bts611
10.1093/bioinformatics/btr381
10.1056/NEJMoa0910812
10.1056/NEJMc1405194
10.1056/NEJMoa1408913
10.1093/cid/ciu313
10.2174/0929867323666161028162018
10.1016/j.ajic.2014.12.020
10.1093/jac/dkp037
10.1086/651706
10.1093/cid/cis338
10.1016/j.medmal.2017.10.007
10.1111/1469-0691.12418
10.1038/nature19799
10.1111/j.1365-2362.2012.02660.x
10.1038/nmicrobiol.2016.30
10.1126/science.aar1999
10.1128/AAC.02176-12
10.7326/M16-2733
10.1093/jac/dku261
10.1128/AEM.01996-06
10.1038/nmeth.f.303
10.1128/JB.00445-10
10.1086/678428
10.1128/AEM.00062-07
10.1097/QCO.0000000000000320
10.1093/jac/dkp042
10.1128/aac.37.1.32
10.1128/AAC.03774-14
10.1016/S1473-3099(17)30235-9
10.1128/AAC.02760-16
10.1097/TA.0000000000001195
10.1016/S1473-3099(11)70374-7
10.1016/j.mib.2018.07.003
10.1086/592257
10.1186/1757-4749-5-23
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Issue 1
Keywords antibiotic
narrow spectrum
phase 1
MAD study
Clostridioides difficile
CRS3123
microbiome
gut microbiota
sporulation
toxin production
Language English
License Copyright © 2019 Lomeli et al.
This is an open-access article distributed under the terms of the Creative Commons Attribution 4.0 International license. https://creativecommons.org/licenses/by/4.0
This is an open-access article distributed under the terms of the Creative Commons Attribution 4.0 International license.
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Citation Lomeli BK, Galbraith H, Schettler J, Saviolakis GA, El-Amin W, Osborn B, Ravel J, Hazleton K, Lozupone CA, Evans RJ, Bell SJ, Ochsner UA, Jarvis TC, Baqar S, Janjic N. 2020. Multiple-ascending-dose phase 1 clinical study of the safety, tolerability, and pharmacokinetics of CRS3123, a narrow-spectrum agent with minimal disruption of normal gut microbiota. Antimicrob Agents Chemother 64:e01395-19. https://doi.org/10.1128/AAC.01395-19.
ORCID 0000-0002-0851-2233
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References e_1_3_3_17_2
e_1_3_3_16_2
e_1_3_3_19_2
Meyers S (e_1_3_3_29_2) 2018; 67
e_1_3_3_38_2
e_1_3_3_18_2
e_1_3_3_39_2
e_1_3_3_13_2
e_1_3_3_36_2
e_1_3_3_12_2
e_1_3_3_37_2
e_1_3_3_15_2
e_1_3_3_34_2
e_1_3_3_14_2
e_1_3_3_35_2
Mercier C (e_1_3_3_48_2) 2013
e_1_3_3_32_2
e_1_3_3_33_2
e_1_3_3_11_2
e_1_3_3_30_2
e_1_3_3_10_2
e_1_3_3_31_2
Tablan OC (e_1_3_3_21_2) 1995; 44
e_1_3_3_40_2
e_1_3_3_6_2
e_1_3_3_5_2
e_1_3_3_8_2
e_1_3_3_7_2
e_1_3_3_28_2
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e_1_3_3_25_2
e_1_3_3_46_2
e_1_3_3_2_2
e_1_3_3_20_2
e_1_3_3_43_2
e_1_3_3_44_2
e_1_3_3_4_2
e_1_3_3_22_2
e_1_3_3_41_2
e_1_3_3_3_2
e_1_3_3_42_2
Vickers, RJ, Tillotson, GS, Nathan, R, Hazan, S, Pullman, J, Lucasti, C, Deck, K, Yacyshyn, B, Maliakkal, B, Pesant, Y, Tejura, B, Roblin, D, Gerding, DN, Wilcox, MH (B37) 2017; 17
Manthey, CF, Eckmann, L, Fuhrmann, V (B13) 2017; 10
Louie, TJ, Miller, MA, Mullane, KM, Weiss, K, Lentnek, A, Golan, Y, Gorbach, S, Sears, P, Shue, YK (B26) 2011; 364
Nayak, SU, Griffiss, JM, Blumer, J, O’Riordan, MA, Gray, W, McKenzie, R, Jurao, RA, An, AT, Le, M, Bell, SJ, Ochsner, UA, Jarvis, TC, Janjic, N, Zenilman, JM (B32) 2017; 61
Lozupone, CA, Hamady, M, Kelley, ST, Knight, R (B48) 2007; 73
Caporaso, JG, Kuczynski, J, Stombaugh, J, Bittinger, K, Bushman, FD, Costello, EK, Fierer, N, Pena, AG, Goodrich, JK, Gordon, JI, Huttley, GA, Kelley, ST, Knights, D, Koenig, JE, Ley, RE, Lozupone, CA, McDonald, D, Muegge, BD, Pirrung, M, Reeder, J, Sevinsky, JR, Turnbaugh, PJ, Walters, WA, Widmann, J, Yatsunenko, T, Zaneveld, J, Knight, R (B43) 2010; 7
Edgar, RC, Haas, BJ, Clemente, JC, Quince, C, Knight, R (B44) 2011; 27
Olsen, MA, Yan, Y, Reske, KA, Zilberberg, MD, Dubberke, ER (B19) 2015; 21
Olsen, MA, Yan, Y, Reske, KA, Zilberberg, M, Dubberke, ER (B18) 2015; 43
Wilcox, MH, Gerding, DN, Poxton, IR, Kelly, C, Nathan, R, Birch, T, Cornely, OA, Rahav, G, Bouza, E, Lee, C, Jenkin, G, Jensen, W, Kim, YS, Yoshida, J, Gabryelski, L, Pedley, A, Eves, K, Tipping, R, Guris, D, Kartsonis, N, Dorr, MB (B7) 2017; 376
Lozupone, CA (B39) 2016; 1
Lessa, FC, Mu, Y, Bamberg, WM, Beldavs, ZG, Dumyati, GK, Dunn, JR, Farley, MM, Holzbauer, SM, Meek, JI, Phipps, EC, Wilson, LE, Winston, LG, Cohen, JA, Limbago, BM, Fridkin, SK, Gerding, DN, McDonald, LC (B4) 2015; 372
Lopetuso, LR, Scaldaferri, F, Petito, V, Gasbarrini, A (B38) 2013; 5
Johnson, S, Louie, TJ, Gerding, DN, Cornely, OA, Chasan-Taber, S, Fitts, D, Gelone, SP, Broom, C, Davidson, DM (B23) 2014; 59
O’Dwyer, K, Spivak, AT, Ingraham, K, Min, S, Holmes, DJ, Jakielaszek, C, Rittenhouse, S, Kwan, AL, Livi, GP, Sathe, G, Thomas, E, Van Horn, S, Miller, LA, Twynholm, M, Tomayko, J, Dalessandro, M, Caltabiano, M, Scangarella-Oman, NE, Brown, JR (B34) 2015; 59
Fadrosh, DW, Ma, B, Gajer, P, Sengamalay, N, Ott, S, Brotman, RM, Ravel, J (B40) 2014; 2
Magill, SS, Edwards, JR, Fridkin, SK (B3) 2014; 370
Debast, SB, Bauer, MP, Kuijper, EJ (B22) 2014; 20
Louie, TJ, Cannon, K, Byrne, B, Emery, J, Ward, L, Eyben, M, Krulicki, W (B36) 2012; 55
Ochsner, UA, Bell, SJ, O’Leary, AL, Hoang, T, Stone, KC, Young, CL, Critchley, IA, Janjic, N (B30) 2009; 63
Goorhuis, A, Bakker, D, Corver, J, Debast, SB, Harmanus, C, Notermans, DW, Bergwerff, AA, Dekker, FW, Kuijper, EJ (B10) 2008; 47
Mercier, C, Boyer, F, Bonin, A, Coissac, E (B47) 2013
Tao, L, Zhang, J, Meraner, P, Tovaglieri, A, Wu, X, Gerhard, R, Zhang, X, Stallcup, WB, Miao, J, He, X, Hurdle, JG, Breault, DT, Brass, AL, Dong, M (B6) 2016; 538
Petrosillo, N (B15) 2018; 48
Tablan, OC, Tenover, FC, Martone, WJ, Gaynes, RP, Jarvis, WR, Favero, MS, Shaw, J (B20) 1995; 44
McDonald, LC, Gerding, DN, Johnson, S, Bakken, JS, Carroll, KC, Coffin, SE, Dubberke, ER, Garey, KW, Gould, CV, Kelly, C, Loo, V, Shaklee Sammons, J, Sandora, TJ, Wilcox, MH (B1) 2018; 66
Merrigan, M, Venugopal, A, Mallozzi, M, Roxas, B, Viswanathan, VK, Johnson, S, Gerding, DN, Vedantam, G (B11) 2010; 192
Ma, GK, Brensinger, CM, Wu, Q, Lewis, JD (B17) 2017; 167
Martin, J, Wilcox, M (B14) 2016; 29
Chapman, BC, Moore, HB, Overbey, DM, Morton, AP, Harnke, B, Gerich, ME, Vogel, JD (B27) 2016; 81
Meyers, S, Shih, J, Neher, JO, Safranek, S (B28) 2018; 67
Brown, KA, Khanafer, N, Daneman, N, Fisman, DN (B8) 2013; 57
Wang, Q, Garrity, GM, Tiedje, JM, Cole, JR (B45) 2007; 73
Kriss, M, Hazleton, KZ, Nusbacher, NM, Martin, CG, Lozupone, CA (B35) 2018; 44
Pepin, J, Alary, ME, Valiquette, L, Raiche, E, Ruel, J, Fulop, K, Godin, D, Bourassa, C (B24) 2005; 40
Critchley, IA, Green, LS, Young, CL, Bullard, JM, Evans, RJ, Price, M, Jarvis, TC, Guiles, JW, Janjic, N, Ochsner, UA (B29) 2009; 63
B2
Gilbart, J, Perry, CR, Slocombe, B (B33) 1993; 37
Dubberke, ER, Schaefer, E, Reske, KA, Zilberberg, M, Hollenbeak, CS, Olsen, MA (B16) 2014; 35
Citron, DM, Warren, YA, Tyrrell, KL, Merriam, V, Goldstein, EJ (B31) 2009; 63
Cornely, OA, Nathwani, D, Ivanescu, C, Odufowora-Sita, O, Retsa, P, Odeyemi, IA (B12) 2014; 69
Chen, P, Tao, L, Wang, T, Zhang, J, He, A, Lam, KH, Liu, Z, He, X, Perry, K, Dong, M, Jin, R (B5) 2018; 360
Flores, R, Shi, J, Gail, MH, Gajer, P, Ravel, J, Goedert, JJ (B41) 2012; 42
Flores, R, Shi, J, Gail, MH, Ravel, J, Goedert, JJ (B42) 2012; 42
Cohen, SH, Gerding, DN, Johnson, S, Kelly, CP, Loo, VG, McDonald, LC, Pepin, J, Wilcox, MH (B21) 2010; 31
Cornely, OA, Crook, DW, Esposito, R, Poirier, A, Somero, MS, Weiss, K, Sears, P, Gorbach, S (B25) 2012; 12
Peretz, A, Shlomo, IB, Nitzan, O, Bonavina, L, Schaffer, PM, Schaffer, M (B9) 2016; 23
Kopylova, E, Noe, L, Touzet, H (B46) 2012; 28
References_xml – ident: e_1_3_3_14_2
  doi: 10.1080/17512433.2017.1362978
– ident: e_1_3_3_25_2
  doi: 10.1086/430315
– ident: e_1_3_3_20_2
  doi: 10.1016/j.cmi.2014.08.017
– ident: e_1_3_3_2_2
  doi: 10.1093/cid/cix1085
– ident: e_1_3_3_41_2
  doi: 10.1186/2049-2618-2-6
– ident: e_1_3_3_42_2
  doi: 10.1111/j.1365-2362.2012.02659.x
– ident: e_1_3_3_8_2
  doi: 10.1056/NEJMoa1602615
– ident: e_1_3_3_3_2
– ident: e_1_3_3_30_2
  doi: 10.1093/jac/dkp041
– ident: e_1_3_3_47_2
  doi: 10.1093/bioinformatics/bts611
– ident: e_1_3_3_45_2
  doi: 10.1093/bioinformatics/btr381
– ident: e_1_3_3_27_2
  doi: 10.1056/NEJMoa0910812
– ident: e_1_3_3_4_2
  doi: 10.1056/NEJMc1405194
– ident: e_1_3_3_5_2
  doi: 10.1056/NEJMoa1408913
– ident: e_1_3_3_24_2
  doi: 10.1093/cid/ciu313
– ident: e_1_3_3_10_2
  doi: 10.2174/0929867323666161028162018
– ident: e_1_3_3_19_2
  doi: 10.1016/j.ajic.2014.12.020
– ident: e_1_3_3_32_2
  doi: 10.1093/jac/dkp037
– ident: e_1_3_3_22_2
  doi: 10.1086/651706
– ident: e_1_3_3_37_2
  doi: 10.1093/cid/cis338
– ident: e_1_3_3_16_2
  doi: 10.1016/j.medmal.2017.10.007
– ident: e_1_3_3_23_2
  doi: 10.1111/1469-0691.12418
– ident: e_1_3_3_7_2
  doi: 10.1038/nature19799
– ident: e_1_3_3_43_2
  doi: 10.1111/j.1365-2362.2012.02660.x
– volume: 67
  start-page: 386
  year: 2018
  ident: e_1_3_3_29_2
  article-title: Clinical inquiries: how effective and safe is fecal microbial transplant in preventing C difficile recurrence?
  publication-title: J Fam Pract
– ident: e_1_3_3_40_2
  doi: 10.1038/nmicrobiol.2016.30
– ident: e_1_3_3_6_2
  doi: 10.1126/science.aar1999
– start-page: 27
  volume-title: Programs Abstr SeqBio
  year: 2013
  ident: e_1_3_3_48_2
– ident: e_1_3_3_9_2
  doi: 10.1128/AAC.02176-12
– ident: e_1_3_3_18_2
  doi: 10.7326/M16-2733
– ident: e_1_3_3_13_2
  doi: 10.1093/jac/dku261
– ident: e_1_3_3_49_2
  doi: 10.1128/AEM.01996-06
– ident: e_1_3_3_44_2
  doi: 10.1038/nmeth.f.303
– ident: e_1_3_3_12_2
  doi: 10.1128/JB.00445-10
– ident: e_1_3_3_17_2
  doi: 10.1086/678428
– ident: e_1_3_3_46_2
  doi: 10.1128/AEM.00062-07
– ident: e_1_3_3_15_2
  doi: 10.1097/QCO.0000000000000320
– ident: e_1_3_3_31_2
  doi: 10.1093/jac/dkp042
– ident: e_1_3_3_34_2
  doi: 10.1128/aac.37.1.32
– ident: e_1_3_3_35_2
  doi: 10.1128/AAC.03774-14
– ident: e_1_3_3_38_2
  doi: 10.1016/S1473-3099(17)30235-9
– ident: e_1_3_3_33_2
  doi: 10.1128/AAC.02760-16
– ident: e_1_3_3_28_2
  doi: 10.1097/TA.0000000000001195
– ident: e_1_3_3_26_2
  doi: 10.1016/S1473-3099(11)70374-7
– ident: e_1_3_3_36_2
  doi: 10.1016/j.mib.2018.07.003
– ident: e_1_3_3_11_2
  doi: 10.1086/592257
– ident: e_1_3_3_39_2
  doi: 10.1186/1757-4749-5-23
– volume: 44
  start-page: 1
  issue: 12
  year: 1995
  ident: e_1_3_3_21_2
  article-title: Recommendations for preventing the spread of vancomycin resistance
  publication-title: MMWR Recommend Rep
– volume: 35
  start-page: 1400
  year: 2014
  end-page: 1407
  ident: B16
  article-title: Attributable inpatient costs of recurrent Clostridium difficile infections
  publication-title: Infect Control Hosp Epidemiol
  doi: 10.1086/678428
– volume: 20
  start-page: 1
  year: 2014
  end-page: 26
  ident: B22
  article-title: European Society of Clinical Microbiology and Infectious Diseases: update of the treatment guidance document for Clostridium difficile infection
  publication-title: Clin Microbiol Infect
  doi: 10.1111/1469-0691.12418
– volume: 17
  start-page: 735
  year: 2017
  end-page: 744
  ident: B37
  article-title: Efficacy and safety of ridinilazole compared with vancomycin for the treatment of Clostridium difficile infection: a phase 2, randomised, double-blind, active-controlled, non-inferiority study
  publication-title: Lancet Infect Dis
  doi: 10.1016/S1473-3099(17)30235-9
– volume: 40
  start-page: 1591
  year: 2005
  end-page: 1597
  ident: B24
  article-title: Increasing risk of relapse after treatment of Clostridium difficile colitis in Quebec, Canada
  publication-title: Clin Infect Dis
  doi: 10.1086/430315
– volume: 42
  start-page: 848
  year: 2012
  end-page: 854
  ident: B42
  article-title: Assessment of the human faecal microbiota: I. Measurement and reproducibility of selected enzymatic activities
  publication-title: Eur J Clin Invest
  doi: 10.1111/j.1365-2362.2012.02660.x
– volume: 538
  start-page: 350
  year: 2016
  end-page: 355
  ident: B6
  article-title: Frizzled proteins are colonic epithelial receptors for C. difficile toxin B
  publication-title: Nature
  doi: 10.1038/nature19799
– volume: 47
  start-page: 1162
  year: 2008
  end-page: 1170
  ident: B10
  article-title: Emergence of Clostridium difficile infection due to a new hypervirulent strain, polymerase chain reaction ribotype 078
  publication-title: Clin Infect Dis
  doi: 10.1086/592257
– volume: 63
  start-page: 972
  year: 2009
  end-page: 976
  ident: B31
  article-title: Comparative in vitro activity of REP3123 against Clostridium difficile and other anaerobic intestinal bacteria
  publication-title: J Antimicrob Chemother
  doi: 10.1093/jac/dkp037
– volume: 21
  start-page: 164
  year: 2015
  end-page: 170
  ident: B19
  article-title: Recurrent Clostridium difficile infection is associated with increased mortality
  publication-title: Clin Microbiol Infect
  doi: 10.1016/j.cmi.2014.08.017
– volume: 28
  start-page: 3211
  year: 2012
  end-page: 3217
  ident: B46
  article-title: SortMeRNA: fast and accurate filtering of ribosomal RNAs in metatranscriptomic data
  publication-title: Bioinformatics
  doi: 10.1093/bioinformatics/bts611
– volume: 73
  start-page: 1576
  year: 2007
  end-page: 1585
  ident: B48
  article-title: Quantitative and qualitative beta diversity measures lead to different insights into factors that structure microbial communities
  publication-title: Appl Environ Microbiol
  doi: 10.1128/AEM.01996-06
– volume: 37
  start-page: 32
  year: 1993
  end-page: 38
  ident: B33
  article-title: High-level mupirocin resistance in Staphylococcus aureus: evidence for two distinct isoleucyl-tRNA synthetases
  publication-title: Antimicrob Agents Chemother
  doi: 10.1128/aac.37.1.32
– volume: 63
  start-page: 954
  year: 2009
  end-page: 963
  ident: B29
  article-title: Spectrum of activity and mode of action of REP3123, a new antibiotic to treat Clostridium difficile infections
  publication-title: J Antimicrob Chemother
  doi: 10.1093/jac/dkp041
– volume: 59
  start-page: 289
  year: 2015
  end-page: 298
  ident: B34
  article-title: Bacterial resistance to leucyl-tRNA synthetase inhibitor GSK2251052 develops during treatment of complicated urinary tract infections
  publication-title: Antimicrob Agents Chemother
  doi: 10.1128/AAC.03774-14
– volume: 10
  start-page: 1239
  year: 2017
  end-page: 1250
  ident: B13
  article-title: Therapy for Clostridium difficile infection—any news beyond metronidazole and vancomycin?
  publication-title: Expert Rev Clin Pharmacol
  doi: 10.1080/17512433.2017.1362978
– volume: 67
  start-page: 386
  year: 2018
  end-page: 388
  ident: B28
  article-title: Clinical inquiries: how effective and safe is fecal microbial transplant in preventing C difficile recurrence?
  publication-title: J Fam Pract
– volume: 43
  start-page: 318
  year: 2015
  end-page: 322
  ident: B18
  article-title: Impact of Clostridium difficile recurrence on hospital readmissions
  publication-title: Am J Infect Control
  doi: 10.1016/j.ajic.2014.12.020
– volume: 81
  start-page: 756
  year: 2016
  end-page: 764
  ident: B27
  article-title: Fecal microbiota transplant in patients with Clostridium difficile infection: a systematic review
  publication-title: J Trauma Acute Care Surg
  doi: 10.1097/TA.0000000000001195
– volume: 364
  start-page: 422
  year: 2011
  end-page: 431
  ident: B26
  article-title: Fidaxomicin versus vancomycin for Clostridium difficile infection
  publication-title: N Engl J Med
  doi: 10.1056/NEJMoa0910812
– volume: 42
  start-page: 855
  year: 2012
  end-page: 863
  ident: B41
  article-title: Assessment of the human faecal microbiota: II. Reproducibility and associations of 16S rRNA pyrosequences
  publication-title: Eur J Clin Invest
  doi: 10.1111/j.1365-2362.2012.02659.x
– volume: 7
  start-page: 335
  year: 2010
  end-page: 336
  ident: B43
  article-title: QIIME allows analysis of high-throughput community sequencing data
  publication-title: Nat Methods
  doi: 10.1038/nmeth.f.303
– ident: B2
  article-title: CDC . 2015 . Nearly half a million Americans suffered from Clostridium difficile infections in a single year . https://www.cdc.gov/media/releases/2015/p0225-clostridium-difficile.html .
– volume: 5
  start-page: 23
  year: 2013
  ident: B38
  article-title: Commensal clostridia: leading players in the maintenance of gut homeostasis
  publication-title: Gut Pathog
  doi: 10.1186/1757-4749-5-23
– volume: 66
  start-page: e1
  year: 2018
  end-page: e48
  ident: B1
  article-title: Clinical practice guidelines for Clostridium difficile infection in adults and children: 2017 update by the Infectious Diseases Society of America (IDSA) and Society for Healthcare Epidemiology of America (SHEA)
  publication-title: Clin Infect Dis
  doi: 10.1093/cid/cix1085
– volume: 370
  start-page: 2542
  year: 2014
  end-page: 2543
  ident: B3
  article-title: Survey of health care-associated infections
  publication-title: N Engl J Med
  doi: 10.1056/NEJMc1405194
– volume: 360
  start-page: 664
  year: 2018
  end-page: 669
  ident: B5
  article-title: Structural basis for recognition of frizzled proteins by Clostridium difficile toxin B
  publication-title: Science
  doi: 10.1126/science.aar1999
– volume: 61
  year: 2017
  ident: B32
  article-title: Safety, tolerability, systemic exposure, and metabolism of CRS3123, a methionyl-tRNA synthetase inhibitor developed for treatment of Clostridium difficile, in a phase 1 study
  publication-title: Antimicrob Agents Chemother
  doi: 10.1128/AAC.02760-16
– volume: 167
  start-page: 152
  year: 2017
  end-page: 158
  ident: B17
  article-title: Increasing incidence of multiply recurrent Clostridium difficile infection in the United States: a cohort study
  publication-title: Ann Intern Med
  doi: 10.7326/M16-2733
– volume: 44
  start-page: 1
  issue: (RR-12)
  year: 1995
  end-page: 13
  ident: B20
  article-title: Recommendations for preventing the spread of vancomycin resistance
  publication-title: MMWR Recommend Rep
– volume: 69
  start-page: 2892
  year: 2014
  end-page: 2900
  ident: B12
  article-title: Clinical efficacy of fidaxomicin compared with vancomycin and metronidazole in Clostridium difficile infections: a meta-analysis and indirect treatment comparison
  publication-title: J Antimicrob Chemother
  doi: 10.1093/jac/dku261
– volume: 12
  start-page: 281
  year: 2012
  end-page: 289
  ident: B25
  article-title: Fidaxomicin versus vancomycin for infection with Clostridium difficile in Europe, Canada, and the USA: a double-blind, non-inferiority, randomised controlled trial
  publication-title: Lancet Infect Dis
  doi: 10.1016/S1473-3099(11)70374-7
– volume: 63
  start-page: 964
  year: 2009
  end-page: 971
  ident: B30
  article-title: Inhibitory effect of REP3123 on toxin and spore formation in Clostridium difficile, and in vivo efficacy in a hamster gastrointestinal infection model
  publication-title: J Antimicrob Chemother
  doi: 10.1093/jac/dkp042
– volume: 55
  start-page: S132
  year: 2012
  end-page: S142
  ident: B36
  article-title: Fidaxomicin preserves the intestinal microbiome during and after treatment of Clostridium difficile infection (CDI) and reduces both toxin reexpression and recurrence of CDI
  publication-title: Clin Infect Dis
  doi: 10.1093/cid/cis338
– volume: 372
  start-page: 825
  year: 2015
  end-page: 834
  ident: B4
  article-title: Burden of Clostridium difficile infection in the United States
  publication-title: N Engl J Med
  doi: 10.1056/NEJMoa1408913
– volume: 376
  start-page: 305
  year: 2017
  end-page: 317
  ident: B7
  article-title: Bezlotoxumab for prevention of recurrent Clostridium difficile infection
  publication-title: N Engl J Med
  doi: 10.1056/NEJMoa1602615
– volume: 57
  start-page: 2326
  year: 2013
  end-page: 2332
  ident: B8
  article-title: Meta-analysis of antibiotics and the risk of community-associated Clostridium difficile infection
  publication-title: Antimicrob Agents Chemother
  doi: 10.1128/AAC.02176-12
– volume: 31
  start-page: 431
  year: 2010
  end-page: 455
  ident: B21
  article-title: Clinical practice guidelines for Clostridium difficile infection in adults: 2010 update by the society for healthcare epidemiology of America (SHEA) and the Infectious Diseases Society of America (IDSA)
  publication-title: Infect Control Hosp Epidemiol
  doi: 10.1086/651706
– volume: 73
  start-page: 5261
  year: 2007
  end-page: 5267
  ident: B45
  article-title: Naive Bayesian classifier for rapid assignment of rRNA sequences into the new bacterial taxonomy
  publication-title: Appl Environ Microbiol
  doi: 10.1128/AEM.00062-07
– volume: 48
  start-page: 18
  year: 2018
  end-page: 22
  ident: B15
  article-title: Tackling the recurrence of Clostridium difficile infection
  publication-title: Med Mal Infect
  doi: 10.1016/j.medmal.2017.10.007
– volume: 27
  start-page: 2194
  year: 2011
  end-page: 2200
  ident: B44
  article-title: UCHIME improves sensitivity and speed of chimera detection
  publication-title: Bioinformatics
  doi: 10.1093/bioinformatics/btr381
– volume: 192
  start-page: 4904
  year: 2010
  end-page: 4911
  ident: B11
  article-title: Human hypervirulent Clostridium difficile strains exhibit increased sporulation as well as robust toxin production
  publication-title: J Bacteriol
  doi: 10.1128/JB.00445-10
– volume: 1
  start-page: 16030
  year: 2016
  ident: B39
  article-title: Getting to know the microbiome
  publication-title: Nat Microbiol
  doi: 10.1038/nmicrobiol.2016.30
– volume: 2
  start-page: 6
  year: 2014
  ident: B40
  article-title: An improved dual-indexing approach for multiplexed 16S rRNA gene sequencing on the Illumina MiSeq platform
  publication-title: Microbiome
  doi: 10.1186/2049-2618-2-6
– start-page: 27
  year: 2013
  end-page: 29
  ident: B47
  article-title: SUMATRA and SUMACLUST: fast and exact comparison and clustering of sequences
  publication-title: Programs Abstr SeqBio
– volume: 59
  start-page: 345
  year: 2014
  end-page: 354
  ident: B23
  article-title: Vancomycin, metronidazole, or tolevamer for Clostridium difficile infection: results from two multinational, randomized, controlled trials
  publication-title: Clin Infect Dis
  doi: 10.1093/cid/ciu313
– volume: 23
  start-page: 4442
  year: 2016
  end-page: 4449
  ident: B9
  article-title: Clostridium difficile infection: associations with chemotherapy, radiation therapy, and targeting therapy treatments
  publication-title: Curr Med Chem
  doi: 10.2174/0929867323666161028162018
– volume: 44
  start-page: 34
  year: 2018
  end-page: 40
  ident: B35
  article-title: Low diversity gut microbiota dysbiosis: drivers, functional implications and recovery
  publication-title: Curr Opin Microbiol
  doi: 10.1016/j.mib.2018.07.003
– volume: 29
  start-page: 546
  year: 2016
  end-page: 554
  ident: B14
  article-title: New and emerging therapies for Clostridium difficile infection
  publication-title: Curr Opin Infect Dis
  doi: 10.1097/QCO.0000000000000320
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Snippet CRS3123 is a novel small molecule that potently inhibits methionyl-tRNA synthetase of Clostridioides difficile , inhibiting C. difficile toxin production and...
CRS3123 is a novel small molecule that potently inhibits methionyl-tRNA synthetase of , inhibiting toxin production and spore formation. CRS3123 has been...
CRS3123 is a novel small molecule that potently inhibits methionyl-tRNA synthetase of Clostridioides difficile, inhibiting C. difficile toxin production and...
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SubjectTerms Administration, Oral
Adolescent
Adult
Anti-Bacterial Agents - administration & dosage
Anti-Bacterial Agents - adverse effects
Anti-Bacterial Agents - pharmacokinetics
Benzopyrans - administration & dosage
Benzopyrans - adverse effects
Benzopyrans - pharmacokinetics
Clostridioides difficile - drug effects
Clostridioides difficile - enzymology
Clostridioides difficile - genetics
Clostridium Infections - drug therapy
Cohort Studies
Dose-Response Relationship, Drug
Double-Blind Method
Drug Administration Schedule
Electrocardiography
Enzyme Inhibitors - administration & dosage
Enzyme Inhibitors - adverse effects
Enzyme Inhibitors - pharmacokinetics
Experimental Therapeutics
Female
Gastrointestinal Microbiome - drug effects
Healthy Volunteers
Humans
Male
Methionine-tRNA Ligase - antagonists & inhibitors
Methionine-tRNA Ligase - genetics
Microbial Sensitivity Tests
Middle Aged
Thiophenes - administration & dosage
Thiophenes - adverse effects
Thiophenes - pharmacokinetics
Young Adult
Title Multiple-Ascending-Dose Phase 1 Clinical Study of the Safety, Tolerability, and Pharmacokinetics of CRS3123, a Narrow-Spectrum Agent with Minimal Disruption of Normal Gut Microbiota
URI https://www.ncbi.nlm.nih.gov/pubmed/31685472
https://journals.asm.org/doi/10.1128/AAC.01395-19
https://www.proquest.com/docview/2312281132
https://pubmed.ncbi.nlm.nih.gov/PMC7187627
https://aac.asm.org/content/aac/64/1/e01395-19.full.pdf
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