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BV100 (rifabutin for infusion) showed dose-proportional pharmacokinetics and safety in healthy volunteersA New IV Drug Targets the Hardest Hospital Infections to Treat

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Key Takeaway
Consider BV100 (rifabutin for infusion) for carbapenem-resistant infections, noting higher adverse events at higher doses with q24h intervals.

This Phase 1 randomized controlled trial assessed the pharmacokinetics, safety, and tolerability of BV100, a formulation of rifabutin for infusion, in a population of healthy volunteers. The sample size was not reported, and the specific setting was not reported in the available data. The intervention involved single-ascending and multiple-ascending doses of BV100. No comparator was explicitly reported for the primary analysis in the provided text.

Regarding the main results, the study demonstrated a dose-proportional pharmacokinetic profile. The half-life of the drug ranged from 7.9 to 56.1 hours, while clearance values ranged from 1.0 to 1.75. When comparing dosing intervals, exposure was 1.5-fold to 2-fold greater with a q12h interval versus a q24h interval. Metabolite activity was observed to be less than 5% of rifabutin activity. Exact absolute numbers and p-values were not reported for these specific outcomes.

Safety and tolerability data indicated that the treatment was generally safe and well tolerated. Adverse events included infusion site events and systemic treatment-emergent adverse events. Serious adverse events were not reported, and discontinuations were not reported. The frequency of adverse events was noted to be higher at higher doses, particularly with the q24h dosing interval and a 60-minute infusion time.

Key limitations include the lack of reported sample size, setting, and specific statistical measures such as confidence intervals or p-values. The study population consisted of healthy volunteers, which limits the direct applicability to patients with carbapenem-resistant infections. The practice relevance notes that BV100 doses of 200-300 mg q12h are currently being evaluated in a Phase 2 study for treating carbapenem-resistant infections. Funding sources and conflicts of interest were not reported.

When the strongest antibiotics stop working

Carbapenems are some of the most powerful antibiotics doctors have. They're often saved for the worst infections, when other drugs have already failed.

But over the last decade, certain hospital bacteria have learned to defeat carbapenems too. When that happens, options narrow fast.

A new clinical study tests an intravenous version of an old drug as one possible answer.

Carbapenem-resistant infections are among the most urgent threats in modern hospitals. The bacteria can cause pneumonia, bloodstream infections, and severe wound infections. Mortality rates are high — sometimes one in three patients — partly because there are so few drugs left that work.

The pharmaceutical pipeline for new antibiotics has slowed for years. Reformulating older drugs that still work against resistant bacteria is one of the more practical near-term strategies.

That's the idea behind BV100.

The old way versus the new way

Rifabutin has been used for decades, mostly in oral form, to treat tuberculosis and certain other infections. It works against some carbapenem-resistant bacteria, but the oral version doesn't reach high enough blood levels quickly to handle severe, fast-moving infections.

BV100 changes that by delivering rifabutin intravenously. Doctors can get high blood concentrations within hours and adjust the dose in real time — exactly what's needed when a patient is critically ill.

The Phase 1 trial reported here is the first careful look at how the IV version behaves in healthy people.

Imagine trying to put out a fast-moving fire by sprinkling water from a watering can. The water reaches the flames, but slowly. A fire hose delivers the same water with much more force and timing.

Oral rifabutin is the watering can. BV100 is the fire hose. Same active medicine, very different delivery. The IV route lets doctors control exactly how much drug a patient gets and how quickly. That control is critical when bacteria are doubling every 30 minutes.

The study snapshot

The team ran two complementary trials. One tested single ascending doses — giving healthy volunteers one dose at increasing strengths to see how the body handles it. The other tested multiple ascending doses, where the same volunteers received the drug repeatedly over several days at different intervals. Blood samples tracked drug concentration and broke down how the body processed it. Volunteers were also closely monitored for side effects.

BV100 behaved predictably. As doses went up, blood levels rose proportionally. The drug stayed in the system long enough to support either once-daily or twice-daily dosing, and twice-daily dosing produced the higher overall exposure expected from any drug given more often.

The medicine's main breakdown product made up less than 5% of total activity, suggesting it doesn't significantly add to either effectiveness or risk.

Side effects were what doctors would have predicted from rifabutin's long history. The most common issue was reactions at the infusion site, more frequent at higher doses and longer infusion times. No new safety problems came up.

Based on these results, doses of 200 to 300 mg every 12 hours have moved into Phase 2 testing in patients with actual carbapenem-resistant infections.

This was a healthy-volunteer study, not a trial showing patients got better.

Where this fits in the bigger picture

Drug-resistant infections kill more than a million people worldwide each year. Most new antibiotic candidates either fail in trials or take a decade to reach patients. Reformulating drugs that already work — like rifabutin — offers a faster way to expand the toolkit.

If BV100 holds up in the next phase of testing, it joins a small but important group of newer agents available for the hardest hospital infections.

If you or a family member ends up hospitalized with a serious infection, you don't need to know the name of any specific drug. Hospital infectious-disease teams choose antibiotics based on the bacteria identified and what's known to still work against them.

The bigger takeaway is for everyone. Antibiotic resistance is a slow-moving emergency. Using antibiotics only when truly needed — not for every cold or sore throat — helps preserve the ones we still have, including the next generation in development.

Phase 1 trials are designed to test safety, not whether the drug actually cures infections. The participants here were healthy adults, not critically ill patients with resistant bacteria. Real-world dosing may need to be different in patients with kidney or liver problems, or those taking other medications. The infusion-site reactions also need to be looked at carefully in sicker patients.

A Phase 2 trial is now testing BV100 at the recommended doses in patients with carbapenem-resistant infections. That study will measure both safety and clinical response. If the results are encouraging, larger trials will follow. The whole process typically takes several years before a drug becomes widely available — but the urgent need for new options against resistant infections is keeping the pace moving.

Study Details

Study typeRct
EvidenceLevel 2
PublishedApr 2026
View Original Abstract ↓
BV100 (rifabutin for infusion) is being developed as an intravenous formulation for treating serious or life-threatening infections due to carbapenem-resistant in patients with limited treatment options. Phase 1 studies were conducted to characterize the pharmacokinetics (PK), safety, and tolerability of BV100 in healthy volunteers after single and multiple doses. Single-ascending and multiple-ascending dose studies were conducted in healthy subjects to establish the PK profile of BV100. Blood samples were assayed to determine plasma concentrations of rifabutin and the major metabolite 25-O-desacetyl-rifabutin and to determine PK parameters. Subjects were assessed for safety and tolerability. The PK profile of BV100 was generally dose-proportional in the single-ascending dose studies with a of 7.9-56.1 h, and of 1.0-1.75 h and increasing exposure with dose. A q12h versus q24h dosing interval resulted in approximately a 1.5-fold to 2-fold greater exposure of rifabutin. The 25-O-desacetyl-rifabutin metabolite represented <5% of rifabutin activity. Adverse events were more common at higher doses with q24h versus q12h dosing, and with a 60 min infusion time. The most common adverse events were infusion site events, with systemic treatment-emergent adverse events as expected for the known safety profile of rifabutin. No other treatment-related safety issues were identified. BV100 demonstrated a dose-proportional PK profile and was generally safe and well tolerated. Based on these results, BV100 doses of 200-300 mg q12h are undergoing evaluation in a Phase 2 study for treating carbapenem-resistant infections.CLINICAL TRIALSThis study is registered with ClinicalTrials.gov as NCT04636983 and NCT05087069.
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