Safety, Tolerability, Pharmacokinetics of Intravenous RPX2003 (Biapenem) in Healthy Adult Subjects

The worldwide spread of resistance to antibiotics among Gram-negative bacteria, particularly
members of the ESKAPE group of pathogens, has resulted in a crisis in the treatment of
hospital acquired infections. In particular, the recent dissemination of a serine
carbapenemase (e.g., KPC) in Enterobacteriaceae in US hospitals now poses a considerable
threat to the carbapenems and other members of the beta-lactam class of antimicrobial
agents.

Rempex is developing a fixed combination antibiotic of a carbapenem (RPX2003 or biapenem)
plus a new beta-lactamase inhibitor (RPX7009) which has activity against serine
beta-lactamases, including KPC. This Phase 1 study will assess the safety, tolerability and
pharmacokinetics of biapenem, administered alone, in healthy adult subjects.

Inclusion Criteria:

- Healthy adult males and/or females, 18 to 55 years of age

- Body mass index (BMI) ≥ 18.5 and ≤ 29.9 (kg/m2) and weight between 55.0 and 100.0
kg (inclusive).

- Medically healthy with clinically insignificant screening results

- Non-tobacco/nicotine-containing product users for a minimum of 6 months prior to Day
1.

- Sexually abstinent or use acceptable methods of birth control

Exclusion Criteria:

- History or presence of significant cardiovascular, pulmonary, hepatic, renal,
hematological, gastrointestinal, endocrine, immunologic, dermatologic, neurological,
or psychiatric disease.

- History or presence of alcoholism or drug abuse within the 2 years prior to Day 1.

- Hypersensitivity or idiosyncratic reaction to compounds related to the study drug
(e.g. beta-lactam antibiotics such as penicillins, carbapenems, etc).

- History of seizures (e.g., epilepsy).

- Use of any over-the-counter (OTC) medication, including herbal products and vitamins,
within the 7 days prior to Day 1. Up to 2 grams per day of acetaminophen is allowed
for acute events at the discretion of the PI.

- Blood donation or significant blood loss (i.e., > 500 mL) within 56 days prior to Day
1.

- Subjects who have any abnormalities on laboratory values at screening or check-in
(Day -1).