OBE002 / ObsEva - LARVOL DELTA

Co-administration of the prostaglandin F2α receptor antagonist pre-term labour drug candidate OBE022 with magnesium sulfate, atosiban, nifedipine and betamethasone. (PubMed, Br J Clin Pharmacol) - "The use of OBE022, a PGF2α antagonist prodrug, in combination with standard-of-care medicines may provide new treatment alternatives for pre-term labour. All tested combinations were well tolerated. Nifedipine doses could potentially be reduced or staggered when co-administered with OBE022."

Journal

Confirmation of the Cardiac Safety of PGFReceptor Antagonist OBE022 in a First-in-Human Study in Healthy Subjects, Using Intensive ECG Assessments. (PubMed, Clin Pharmacol Drug Dev) - "Concentration-effect modeling was used to assess the effect of prodrug OBE022 and parent OBE002 on QTc after a single dose (days 1 and 3) and multiple doses (day 9)...The observed food effect on the QT interval validated the assay on all assessment days. Both the change from predose, premeal and the change from premeal, postdose demonstrated the specificity of the method."

Clinical • Journal • P1 data

Pharmacokinetics, safety and tolerability of OBE022, a selective prostaglandin F2α receptor antagonist tocolytic: A First-in-human trial in healthy post-menopausal women. (PubMed, Br J Clin Pharmacol) - "Administration of OBE022 was safe and had favourable pharmacokinetic characteristics and no clinically relevant interaction with food. Our results allow further investigation of OBE022 in preterm labour patients."

Clinical • Journal • P1 data • PK/PD data

OBE022, an oral and selective prostaglandin F2α receptor antagonist as an effective and safe modality for the treatment of preterm labor. (PubMed, J Pharmacol Exp Ther) - "In pregnant mice, OBE022 delayed RU486 [(8S,11R,13S,14S,17S)-11-[4-(dimethylamino)phenyl]-17-hydroxy-13-methyl-17-prop-1-ynyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one] -induced parturition and exerted synergistic effects in combination with nifedipine. Orally active OBE022 and OBE002 exhibits potent tocolytic effects on human tissues ex vivo and animal models in vivo without causing the adverse fetal side effects seen with indomethacin. Selectively targeting the FP receptor in combination with existing tocolytics may be an effective strategy for preventing or delaying preterm delivery."

Journal