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ADVANCING NEW CLASSES OF MEDICINES FOR A RANGE OF IMPORTANT DISEASES

Our pipeline reflects a focused strategy to advance innovative boron-based therapeutics across infectious disease and oncology indications. Each program is designed to address significant unmet medical needs with differentiated chemistry and a strong mechanistic rationale.

Product Name Target/Mechanism Research Preclinical Phase 1 Phase 2 Pivotal

Epetraborole (EBO)

Polycythemia vera
Globin synthesis
Phase 2
M. abscessus lung disease
LeuRS
Phase 2
Melioidosis
LeuRS
Phase 2

AN2-502998

Chagas disease
CPSF3
Phase 2

Research Programs

Oncology
РІЗК𝛼
Pre-Clinical
Oncology
ENPP1
Pre-Clinical
Bone disorders
ENPP1
Research
Tuberculosis
LeuRS
Research
Polycythemia vera

Polycythemia vera (PV) is a rare, chronic myeloproliferative neoplasm characterized by the overproduction of red blood cells and is caused in the vast majority of cases by activating mutations in JAK2. PV significantly increases the risk of thrombosis, cardiovascular complications, and reduced quality of life, and many patients remain dependent on regular phlebotomy to control hematocrit levels. Over time, patients may progress to myelofibrosis or acute myeloid leukemia, conditions associated with substantial morbidity and mortality.

Epetraborole, an oral, small-molecule therapy, offers a novel mechanism in PV by targeting globin synthesis. Prior clinical data in non-PV patients indicate potential for dose-dependent, reversible hematocrit reductions without broadly suppressing white cells or platelets—a profile consistent with red-cell selectivity rather than generalized cytoreduction—and without the iron deficiency seen with phlebotomy.

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Chagas disease

Chagas disease is caused by T. cruzi and affects an estimated 300,000 people in the US (7-10 million worldwide). Local transmission is increasing due to the spread of “kissing bugs,” which are now present in at least 32 states. Twenty to thirty percent of people infected will develop severe cardiac or gastrointestinal disease, and ~30% will progress to Chagas cardiomyopathy, a chronic condition that can lead to sudden death. We are developing AN2-502998, an oral, small molecule benzoxaborole targeting CPSF3 for Chagas disease. Preclinical data show AN2-502998 is potentially curative, has favorable non-clinical safety to date, and kills both actively dividing and dormant parasites faster than benznidazole.

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M. abscessus

M. abscessus affects the lungs and is a CDC-recognized urgent antimicrobial resistance threat. Current standard of care involves multi-drug regimens given for ≥12 months. Treatment success rates are <50%, and there is significant toxicity risk from prolonged antibiotic exposure. We are developing epetraborole (EBO), an oral, boron-based antibiotic for the treatment of M. abscessus. Preclinical data show potent in vitro activity against clinical isolates including macrolide-resistant strains, favorable pharmacokinetic properties supporting oral dosing, synergy with current standard of care agents, and cidal activity in a preclinical lung model.

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Oncology: PI3Kα

PI3Kα is a high value, validated cancer pathway. PIK3CA mutations are among the most common genetic drivers of cancer. These mutations are especially concentrated in three positions: H1047, E542, and E545. Most approved and late-stage PI3Kα inhibitors show strong selectivity only for H1047 mutations. We are working to bring forward a best-in-class, mutant-selective PI3Kα inhibitor that targets the neglected E542 and E545 mutations with high selectivity. Preclinical data show tumor regression without hyperglycemia or hyperinsulinemia, and in vivo efficacy comparable to or exceeding that of alpelisib.

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Immuno-oncology: ENPP1

The immune system detects and attacks cancer in part via a signaling molecule called cGAMP. Damaged cancer cells release cGAMP, which triggers an innate immune response that turns “cold” tumors “hot.” However, an enzyme called ENPP1 can degrade cGAMP and thus silence the alarm signal and protect the tumor. We are developing highly potent, boron-based ENPP1 inhibitors that are intended to help activate the immune system. Preclinical data show single-agent efficacy comparable to PD-1 and CTLA-4 checkpoint inhibitors, synergistic effects when combined with anti-CTLA-4, and durable tumor regression with immune memory.

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Clinical trials

AN2 Therapeutics is committed to delivering high-impact drugs to patients that address critical unmet needs and improve health outcomes. Successful clinical trials are required to gain regulatory approval for new medications to advance patient care and may be required to support any approved products.

 

For information on AN2 Therapeutics clinical trials that may be recruiting, search “AN2 Therapeutics” at www.clinicaltrials.gov.

Presentations and publications