# A Phase Ia/Ib Clinical Study of HIV Entry Inhibitor CPT31:Single and Multiple Ascending Dose Study of Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics in Healthy Adults anAdults with HIV

> **NIH NIH U44** · NAVIGEN, INC. · 2020 · $1,000,000

## Abstract

SUMMARY 
  HIV/AIDS remains a formidable global epidemic, with ~37 million people infected (including ~1.1 million in 
the  US)  and  about  one  million  AIDS-­related  deaths  in  2017  (UNAIDS,  CDC).  Despite  the  efficacy  of  modern 
combination  anti-­retroviral  therapy  (cART),  side  effects  and  drug  resistance  remain  serious  obstacles  to 
achieving  optimal  care,  and  poor  adherence  is  a  key  factor  in  treatment  failure.  Thus,  there  is  continued 
demand  for  well-­tolerated  HIV  inhibitors  with  novel  mechanisms  of  action  and  stronger  barriers  to  resistance. 
HIV specialists are especially enthusiastic about the potential of long-­acting therapies to minimize side effects, 
enhance  efficacy,  and  delay  resistance  through  improved  compliance.    Navigen  has  identified  a  novel, 
protease-­resistant D-­peptide HIV entry inhibitor, CPT31, with these desired characteristics and has advanced it 
through preclinical development. CPT31 addresses many of the limitations of current cART and has proven to 
be  well  tolerated  and  highly  efficacious  for  both  indications  in  non-­human  primates  (NHPs),  making  it  an  ideal 
candidate  for  both  therapy  and  PrEP.  Additionally,  CPT31’s  PK  makes  it  amenable  to  monthly  and  perhaps 
quarterly  dosing  (with  depot  formulation).  In  this  grant  application,  we  will  partner  with  Johns  Hopkins 
University  to  conduct  a  Phase  Ia/Ib  safety,  tolerability,  pharmacokinetics,  and  pharmacodynamics  study  of 
CPT31.  The  study  will  include  three  stages:  1)  single  ascending  dose  (SAD)  in  healthy  volunteers,  2)  multiple 
ascending dose (MAD) in healthy volunteers, and 3) MAD in HIV positive patients classified as Group 1 under 
the  FDA  guidance  for  industry.  This  study  will  enable  Navigen  to  determine  whether  CPT31  has  the 
characteristics that warrant continued clinical studies and further investment.

## Key facts

- **NIH application ID:** 9785192
- **Project number:** 2U44AI095172-08
- **Recipient organization:** NAVIGEN, INC.
- **Principal Investigator:** ALAN L MUELLER
- **Activity code:** U44 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $1,000,000
- **Award type:** 2
- **Project period:** 2011-08-10 → 2023-03-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/9785192

## Citation

> US National Institutes of Health, RePORTER application 9785192, A Phase Ia/Ib Clinical Study of HIV Entry Inhibitor CPT31:Single and Multiple Ascending Dose Study of Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics in Healthy Adults anAdults with HIV (2U44AI095172-08). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/9785192. Licensed CC0.

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