Review 10.1517/14728210802568764฀©฀2008฀Informa฀UK฀Ltd฀ISSN฀1472-8214฀ 1 All฀rights฀reserved:฀reproduction฀in฀whole฀or฀in฀part฀not฀permitted Emerging฀tocolytics:฀challenges฀ in฀designing฀and฀testing฀drugs฀ to฀delay฀preterm฀delivery฀and฀ prolong฀pregnancy David M Olson , Inge Christiaens, Sara Gracie, Yuka Yamamoto & Bryan F Mitchell AHFMR Interdisciplinary Team in Preterm Birth and Healthy Outcomes, Departments of Obstetrics and Gynecology, Pediatrics and Physiology, University of Alberta, Edmonton, Canada The global rate of preterm delivery (before 37 completed weeks of pregnancy) is increasing and there are no effective means available to prevent this rise. Prematurity is the principal cause of neonatal mortality and a major cause of pediatric morbidity and long-term disability. Current strategies to prolong pregnancy are based on inhibiting the mechanisms that effect uterine smooth muscle (myometrium) contractions in women who are in preterm labor. Most drugs in this group were developed for other purposes. Newer strategies are designed to maintain a state of uterine quiescence and preg- nancy, preventing the myometrium from initiating contractions and entering preterm labor. Again, it may be possible to use existing drugs for pregnancy maintenance. Several financial and practical barriers exist for developing completely new drugs to delay labor. Designing clinical trials to test tocolytics is complicated, as the health of two patients must be considered and the nature of preterm birth and its outcomes are different at early preterm labor (< 28 weeks) and late preterm labor (34 – 36 weeks). Keywords: atosiban, morbidity, myometrium, neonatal, NSAIDs, pregnancy, prematurity, preterm birth, preterm labor, progesterone, tocolytics, uterus Expert Opin. Emerging Drugs (2008) 13(4):1-13 1.฀ Background Prematurity is the principal cause of neonatal mortality [1] and a major cause of pediatric morbidity and long-term disability [2-4]; it is associated with at least 50% of all pediatric neurodevelopmental disorders [5]. Infants born preterm (< 37 completed weeks of gestation) are at increased risk for a range of adverse neonatal outcomes, including retinopathy of prematurity [6], respiratory distress syndrome and bronchopulmonary dysplasia [7], severe brain injury [8], necrotizing enterocolitis [9], and neonatal sepsis [10]. Long-term sequelae include risk for motor and sensory impairment (including cerebral palsy, visual impairment, and hearing impairment) [11,12], learning problems and neurocognitive impairment (including lower IQ and lower academic achievement) [13-18], and behavioral problems (e.g., attention deficit hyperactivity disorder, ADHD) [19-24]. Although the risk for mortality and morbidity is higher among early preterm births (< 32 weeks’ gestation), late preterm births (34 to 36 weeks’ gestation) [25] are more common and rates are increasing [26], thus creating a serious public health problem. Recent evidence is demonstrating that late preterm birth infants are also at risk for subtle developmental delays [27]. In spite of approximately 40 years of study and pharmaceutical testing to develop drugs that have the potential to arrest uterine myometrial contractility, 1. Background 2. Medical need 3. Scientific rationale 4. Competitive environment 5. Potential development issues 6. Existing treatment and therapeutic class review 7. Current research goals and emerging treatments 8. Expert opinion 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55