- |||||||||| macozinone (PBTZ169) / Innovative Medicines for Tuberculosis, Nearmedic, Bill & Melinda Gates Foundation
Review, Journal: DprE1 Inhibitors: An insight into the recent developments and synthetic approaches. (Pubmed Central) - May 18, 2025 DprE1 inhibitors can be categorized according to the formation of a covalent or non-covalent bond in the enzyme's active site, causing a loss of its catalytic activity, leading to Mtb's demise. Herein, we describe diverse DprE1 inhibitors that have had anti-tubercular activity reported over the past fifteen years and till the present time.
- |||||||||| 10E8.4/iMab / Bill & Melinda Gates Foundation, IAVI, TaiMed Biologics, VRC07-523LS / National Institute of Allergy and Infectious Diseases, IAVI, TaiMed Biologics
Enrollment closed, Trial completion date, Trial primary completion date: 10E8.4/iMab Bispecific Antibody and VRC07-523LS Monoclonal Antibody in HIV-infected Adults (clinicaltrials.gov) - Apr 25, 2025 P1, N=20, Active, not recruiting, N=732 --> 492 Recruiting --> Active, not recruiting | Trial completion date: Feb 2026 --> May 2027 | Trial primary completion date: May 2025 --> Apr 2026
- |||||||||| Journal: Verapamil and its metabolite norverapamil inhibit the Mycobacterium tuberculosis MmpS5L5 efflux pump to increase bedaquiline activity. (Pubmed Central) - Apr 17, 2025
Here, we show that the MmpS5L5 efflux pump reduces susceptibility to bedaquiline as well as its new, more potent derivative TBAJ-876 and other antimicrobial substrates, including clofazimine and the DprE1 inhibitors PBTZ-169 and OPC-167832...Finally, norverapamil, the major verapamil metabolite, which has greatly reduced calcium channel activity, has equal potency in reducing resistance to MmpS5L5 substrates. Our findings highlight verapamil's potential for enhancing bedaquiline TB treatment, for preventing acquired resistance to bedaquiline and other MmpS5L5 substrates, while also providing the impetus to identify additional MmpS5L5 inhibitors.
- |||||||||| MAM01 / Atreca, Bill & Melinda Gates Foundation
Enrollment open: Study To Evaluate Safety, Tolerability, and Pharmacokinetics of MAM01 in African Population (clinicaltrials.gov) - Apr 4, 2025 P1, N=139, Recruiting, Our findings highlight verapamil's potential for enhancing bedaquiline TB treatment, for preventing acquired resistance to bedaquiline and other MmpS5L5 substrates, while also providing the impetus to identify additional MmpS5L5 inhibitors. Not yet recruiting --> Recruiting
- |||||||||| IMC-M113V / Immunocore, Bill & Melinda Gates Foundation
HIV GAG x CD3 Soluble TCR Bispecific Reduces the Active HIV Reservoir in a Phase I/II Trial (San Francisco Ballroom B) - Mar 3, 2025 - Abstract #CROI2025CROI_124; P1/2 IMC-M113V (GAGxCD3) is the first HIV ImmTAV in the clinic; a single dose study demonstrated safety and biological activity in antiretroviral therapy (ART)-suppressed PLWH...This study provides the first evidence of antiviral efficacy for this novel mechanism of action. Doses >300 ?g and longer ATI duration will be evaluated.
- |||||||||| GSK692342 / GSK, Bill & Melinda Gates Foundation, Sirturo (bedaquiline) / J&J, Pharmstandard
Review, Journal: Tuberculosis: An Update for the Clinician. (Pubmed Central) - Mar 2, 2025 Encouraging clinical results have been seen with the M72/AS01E vaccine...New shorter, all-oral treatment regimens represent a breakthrough, but progress is threatened by rising resistance to bedaquiline...Post-TB lung disease (PTLD) is an under-recognised but growing concern, affecting millions of survivors with lasting respiratory impairment and increased mortality. Continued investment in development of TB vaccines and therapeutics, treatment shortening, and management of TB sequelae is critical to combat this ongoing public health challenge.
- |||||||||| macozinone (PBTZ169) / Innovative Medicines for Tuberculosis, Nearmedic, Bill & Melinda Gates Foundation
Journal: Real-time evaluation of macozinone activity against Mycobacterium tuberculosis through bacterial nanomotion analysis. (Pubmed Central) - Jan 31, 2025 PBTZ169 and H2-PBTZ169 achieved 100% separation between the susceptible H37Rv and a resistant dprE1 mutant strain NTB1. These findings support nanomotion technology's potential for faster antibiotic susceptibility testing of novel MTB drug candidates targeting the DprE1 enzyme that could reduce empirical treatment duration and antibiotic resistance selection pressure due to inaccurate treatments.
- |||||||||| GSK692342 / GSK, Bill & Melinda Gates Foundation
Journal: Strong immune responses and robust protection following a novel protein in adjuvant tuberculosis vaccine candidate. (Pubmed Central) - Jan 14, 2025 M72/AS01E, demonstrated 49.7% efficacy in preventing active TB in latently infected adults, indicating that protective immunity through subunit vaccines is possible...Heterologous vaccination strategies were also explored by combining intranasal ChAdOx1.PPE15 viral vector, with intramuscular PPE15-LMQ resulting in improved protection compared to individual vaccines. These findings support the progression of this vaccine candidate to the next stages of development.
- |||||||||| 10E8.4/iMab / Bill & Melinda Gates Foundation, IAVI, TaiMed Biologics, VRC07-523LS / National Institute of Allergy and Infectious Diseases, IAVI, TaiMed Biologics
Trial completion date, Trial primary completion date: 10E8.4/iMab Bispecific Antibody and VRC07-523LS Monoclonal Antibody in HIV-infected Adults (clinicaltrials.gov) - Jan 10, 2025 P1, N=20, Recruiting, These findings support the progression of this vaccine candidate to the next stages of development. Trial completion date: Feb 2025 --> Feb 2026 | Trial primary completion date: Dec 2024 --> May 2025
- |||||||||| macozinone (PBTZ169) / Innovative Medicines for Tuberculosis, Nearmedic, Bill & Melinda Gates Foundation
Review, Journal: Advances in antibacterial agents for Mycobacterium fortuitum. (Pubmed Central) - Nov 4, 2024 Most compounds effective against M. fortuitum are synthetic, with macozinone, featuring a 2-piperazine-benzothiazinone framework, standing out as a notable drug candidate...Some compounds' mechanisms of action on M. fortuitum have been studied, including NITD-916, which acts as an enoyl-acyl carrier protein reductase inhibitor, and TBAJ-5307, which inhibits F-ATP synthase. Moreover, this review discusses the pathogenic molecular mechanisms and potential therapeutic targets within this mycobacterium.
- |||||||||| MAM01 / Atreca, Bill & Melinda Gates Foundation
Enrollment change, Trial completion date, Trial initiation date, Trial primary completion date: Study To Evaluate Safety, Tolerability, and Pharmacokinetics of MAM01 in African Population (clinicaltrials.gov) - Oct 29, 2024 P1, N=139, Not yet recruiting, Moreover, this review discusses the pathogenic molecular mechanisms and potential therapeutic targets within this mycobacterium. N=264 --> 139 | Trial completion date: May 2026 --> Jan 2026 | Initiation date: Sep 2024 --> Jan 2025 | Trial primary completion date: May 2026 --> Jan 2026
- |||||||||| MAM01 / Atreca, Bill & Melinda Gates Foundation
Trial primary completion date: Safety, Tolerability, Pharmacokinetics and Protective Efficacy of MAM01 in Healthy Adults (clinicaltrials.gov) - Oct 29, 2024 P1, N=61, Recruiting, N=264 --> 139 | Trial completion date: May 2026 --> Jan 2026 | Initiation date: Sep 2024 --> Jan 2025 | Trial primary completion date: May 2026 --> Jan 2026 Trial primary completion date: Mar 2025 --> Dec 2024
- |||||||||| macozinone (PBTZ169) / Innovative Medicines for Tuberculosis, Nearmedic, Bill & Melinda Gates Foundation, Sutezolid (PNU-100480) / Sequella
Efficacy of Macozinone and Sutezolid against Mycobacterium leprae (Convention Center - Hall I-1 (1st Floor); In-Person-Only) - Oct 11, 2024 - Abstract #ASTMH2024ASTMH_2195; Results & Conclusion Results show that Macozinone and Sutezolid are effective against M. lepra e both in vitro (axenic and intracellular) and in vivo (MFP). Therefore, Macozinone and Sutezolid, having different modes of action, should be tested in combination with other first and second line drugs to explore new shorter treatment regimens for leprosy.
- |||||||||| L9LS / National Institute of Allergy and Infectious Diseases, MAM01 / Atreca, Bill & Melinda Gates Foundation
190 - Clinical Development of Monoclonal Antibodies that Target Malaria Sporozoites (Convention Center - Room 393/394 (3rd Floor); In-Person-Only) - Sep 15, 2024 - Abstract #ASTMH2024ASTMH_827; Each presenter will provide an overview on prior experience exploring some of these concepts in prior and current projects, but also will discuss important concepts to explore in future mAb clinical trials. Ample time will be provided at the end of the symposium to promote Q&A and discussion from the audience.
- |||||||||| mRNA based therapeutic / BioNTech, Bill & Melinda Gates Foundation
Preclinical, Review, Journal: Understanding the impact of in vitro transcription byproducts and contaminants. (Pubmed Central) - Jul 26, 2024 The success of messenger (m)RNA-based vaccines against SARS-CoV-2 during the COVID-19 pandemic has led to rapid growth and innovation in the field of mRNA-based therapeutics...In addition, we briefly overview non-nucleotide-based contaminants such as RNases, endotoxin and metal ions that, when present in the IVT reaction, can also influence the activity of mRNA-based drugs. We further discuss current approaches aimed at adjusting the IVT reaction conditions or improving mRNA purification to achieve optimal performance for medical applications.
- |||||||||| TBA-7371 / Bill & Melinda Gates Foundation, Global Alliance for TB Drug Development, Foundation for Neglected Disease Research
Phase classification: Early Bactericidal Activity of TBA-7371 in Pulmonary Tuberculosis (clinicaltrials.gov) - Apr 11, 2024 P2, N=93, Completed, This research lays a strategic foundation for targeted interventions against drug-resistant TB, highlighting ligand 2's potential for advanced drug development strategies. Phase classification: P2a --> P2
- |||||||||| GSK692342 / GSK, Bill & Melinda Gates Foundation
Journal: Momentum of hope: The journey toward a universal TB vaccine. (Pubmed Central) - Apr 2, 2024 Recent developments, such as the M72/AS01E vaccine, demonstrate promising results in increasing protection against TB in adults with latent infections...The pursuit of more effective TB vaccines, capable of providing broader protection across all age groups, is paramount. This effort not only aligns with the WHO's End TB Strategy but also offers hope for a future where TB is no longer a global health crisis.
- |||||||||| 10E8.4/iMab / Bill & Melinda Gates Foundation, IAVI, TaiMed Biologics
10e8.4/iMAb Bispecific Antibody for Immunoprophylaxis Against High-Dose Intravenous SHIV Exposure (Poster hall) - Mar 16, 2024 - Abstract #CROI2024CROI_1094; Not yet recruiting --> Recruiting | Trial completion date: Aug 2029 --> Apr 2028 | Trial primary completion date: Aug 2029 --> Apr 2028 Passive intravenous provision of potent anti-HIV bispecific bNAbs is a highly promising immunoprophylaxis strategy for high-dose intravenous HIV exposure.
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