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Ramoplanin (CAS: 76168-82-6)

Glycolipodepsipeptide Antibiotic

Ramoplanin™ Oral Capsule - Phase 2 clinical program

Ramoplanin™ is a glycolipodepsipeptide antibiotic that is bactericidal for many gram-positive aerobic and anaerobic bacteria, including C. difficile. infection (CDI), vancomycin-resistant enteroccocus (VRE) and methicillin-resistant Staphylococcus aureus (MRSA). Ramoplanin™ has been reported to also have activity against C. difficile spores, both in vitro and in an animal model. The sporicidal mechanism is relatively novel in that the exosporium may be the target for Ramoplanin™ binding, permitting an “ambush” type of vegetative cell killing. The natural history of CDI, regretfully, does not end with successful treatment of the infection. Approximately 25% of patients will experience a recurrence with higher rates among older age groups as well as increasing comorbidities. These relapses are thought to be at least partially due to residual spores in the human gut in clinically cured patients. Elimination of these spores could reduce relapse rates, decreasing the risk of readmission, further treatment requirements, or adverse clinical outcomes. Nanopharmaceutics believes that Ramoplanin™, based on its relatively novel mechanism of action, non-absorbable kinetics (enhanced by dosing to non-inflamed gut mucosa) and established safety profile from prior studies would fill this innovation gap. Twelve phase 1 studies, two phase 2 studies (one in CDI and one in VRE) as well as one phase 3 study (in CDI) have been conducted.


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Doxycycline (CAS: 17086-28-1)

Broad-spectrum antibiotic and anti-inflammatory

NanoDOX® Topical Gel - Phase 2 clinical study


Nanopharmaceutics is developing Doxycycline Monohydrate Hydrogel (NanoDOX®) for the treatment of Atopic Dermatitis and other skin infections. Atopic Dermatitis (AD) a common chronic, relapsing, inflammatory skin disease (up to 20% children and 3-6% adult). AD is characterized by skin barrier disruption & an aberrant immune response (e.g. Th2 polarized) to environmental allergens. So far, AD treatments have targeted inflammation with the widespread use of topical and intermittent use of systemic immunomodulators. Despite its high prevalence, negative effects on quality-of-life and economic burden, there are few effective treatments for AD. Our long-term goal is to develop an alternative treatment option for Atopic Dermatitis.

Doxycycline is a tetracycline antibiotic used systemically to treat inflammatory-dermatologic conditions. Several studies in human and animal models have shown doxycycline has anti-inflammatory and pro-healing properties, mainly by blocking tissue proteolytic activity. A recently completed 6-week pilot study at the UF Health Dermatology Department- Springhill, revealed the safety and clinical efficacy of NanoDOX® Hydrogel in AD. Subjects enrolled in the study (15, 11F and 4 M) applied NanoDOX® Hydrogel 1% once daily at bedtime for total of four weeks (or until complete clearance) on the chosen target eczematous area. Investigational drug was well tolerated, no local or systemic adverse events due to investigational drug were reported during the trial. Notably, a significant clinical improvement was observed from Visit 1 (start of treatment) to visit 2 (14 days treatment) and visit 3 (28 days treatment) respectively. In summary, our clinical trial uncovered the use of a non-systemic doxycycline as a potential novel treatment option for AD.


Inhaled gentamicin (NanoGENT™ inhalation solution) is being developed for delivery directly to the lungs for tuberculosis (TB) and other gram-positive infections. Inhaled gentamicin was tested in a murine model of TB. Aerosolized gentamicin-treated mice showed significantly reduced lung TB loads and fewer granulomas relative to untreated controls. These results suggest that direct delivery of antibiotics to the respiratory system may provide therapeutic benefit to conventional treatment regimens for treatment of pulmonary TB.


NanoFOVIR™ is an inhaled cidofovir solution for non-invasive treatment of pulmonary viral infections. Since transmission of viruses typically occurs through inhalation, usually droplets expressed from the oral, nasal, or pharyngeal mucosa of an infected person, non-invasive anti-viral treatment alternatives with proven agents (cidofovir) are needed. In preliminary studies, pulmonary delivery of NanoFOVIR™ (5mg/kg dose) resulted in a high systemic bioavailability compared to IV administration of cidofovir (1mg/kg), but it was clear that the drug was retained in the lung at least to 8 hours supporting the strategy that inhalation maximizes the tissue concentration at the site of initial viral replication. In other previous studies, inhaled formulations of cidofovir (0.5-5 mg/kg) administered 24 to 48 hours following aerosol exposure of 10^5 pfu (Cowpox, Brighton strain) resulted in 90% and 50% survival in Balb/C mice compared to 50-60% survival for subcutaneous cidofovir administration. Inhaled cidofovir has been shown in multiple studies to be highly efficacious against various pox models, producing long-term activity and retention in the lung tissue compared to injectable adminstration, which results in lower pulmonary levels, possible nephrotoxicity, and requires a health-care worker to implement treatment.