# Remdesivir-bisPropionate, a better derivative of remdesivir against SARS-CoV-2: Comparison of in vitro and in vivo PK/PD Study as well as its therapeutic potential

**Authors:** Ashok Chakraborty, Anil Diwan, Vijetha Chiniga, Vinod Arora, Yogesh Thakur, Jayant Tatake, Rajesh Pandey, Preetam Holkar, Neelam Holkar, Tamer M. Ibrahim, Tamer M. Ibrahim, Tamer M. Ibrahim

PMC · DOI: 10.1371/journal.pone.0324811 · PLOS One · 2026-02-20

## TL;DR

Researchers developed a more stable and effective version of remdesivir, called remdesivir-bisPropionate, which shows better antiviral activity in models.

## Contribution

The novel remdesivir derivative, remdesivir-bisPropionate, is shown to be more stable and effective than existing forms.

## Key findings

- Remdesivir-bisPropionate is more stable in vivo than remdesivir alone.
- Encapsulation in biopolymer NV387 further enhances the stability of remdesivir-bisPropionate.
- Remdesivir-bisPropionate shows increased antiviral activity against NL-63 infection in a rat model.

## Abstract

FDA approved remdesivir, which was though very effective against SARS-corona virus in cell culture system but in human its efficacy was below 10%, as reported. The main reasons are due to the poor stability of remdesivir in presence plasma. In order to increase the protective strength of remdesivir we took couple of approaches, one, to make an alternative but better derivative of remdesivir as remdesivir bis-propionate, and the other is to use our platform- designed biopolymer (NV387) to protect remdesivir compound from degradation in presence of plasma. Here we present our results as: (1) Remdesivir-bP is much more stable in vivo compared to remdesivir alone. (2) Remdesivir-bP when encapsulated within biopolymer, NV387, its stability is further enhanced. (3) The antiviral activity is also increased against NL-63 infection to rat model, compared to naked and/or encapsulated remdesivir. (4) The antiviral efficacy of the remdesivir pro-drug, therefore, can be mathematically drawn as follows: remdesivir-bP-encapsulated > remdesivir-encapsulated > remdesivir-bP > remdesivir.

## Linked entities

- **Chemicals:** remdesivir (PubChem CID 121304016), NL-63 (PubChem CID 11845757)
- **Species:** Rattus norvegicus (taxon 10116)

## Full-text entities

- **Genes:** ERVK-6 (endogenous retrovirus group K member 6, envelope) [NCBI Gene 64006] {aka ERVK6, HERV-K(C7), HERV-K108, K-Rev, c-orf, cORF}, ACE2 (angiotensin converting enzyme 2) [NCBI Gene 59272] {aka ACEH}, ANPEP (alanyl aminopeptidase, membrane) [NCBI Gene 290] {aka AP-M, AP-N, APN, CD13, GP150, LAP1}
- **Diseases:** lung infection (MESH:D012141), inflammation (MESH:D007249), ORCID iD (MESH:C535742), lung damage (MESH:D008171), pneumonia (MESH:D011014), nausea (MESH:D009325), ARDS (MESH:D012128), loss of body weight (MESH:D001835), viral infection (MESH:D014777), death (MESH:D003643), Toxicity (MESH:D064420), COVID (MESH:D000086382), immune-compromised (MESH:D007154), Infection (MESH:D007239), allergic reactions (MESH:D004342), renal dysfunction (MESH:D007674), SARS (MESH:D045169), bronchiolitis (MESH:D001988), septic shock (MESH:D012772)
- **Chemicals:** Favipiravir (MESH:C462182), GS-441524 (MESH:C000710751), azithromycin (MESH:D017963), adenosine (MESH:D000241), GS-441524-MP (MESH:C000718587), GS-5734 (MESH:C000606551), sodium pentobarbital (MESH:D010424), acetonitrile (MESH:C032159), ester (MESH:D004952), GS-704277 (MESH:C000722731), propionic acid (MESH:C029658), Ribavirin (MESH:D012254), fluorouracil (MESH:D005472), water (MESH:D014867), EtOH (MESH:D000431), acyclovir (MESH:D000212), anidulafungin (MESH:D000077612), triphosphate (MESH:C005692), H&amp;E (MESH:D006371), lopinavir (MESH:D061466), NV-387 (-), GS-443902 (MESH:C000706175), CO2 (MESH:D002245), ATP (MESH:D000255), propionic anhydride (MESH:C096126), 4-Dimethylaminopyridine (MESH:C003885), DMSO (MESH:D004121)
- **Species:** Severe acute respiratory syndrome coronavirus 2 (no rank) [taxon 2697049], Gammacoronavirus (genus) [taxon 694013], Severe acute respiratory syndrome-related coronavirus (no rank) [taxon 694009], Human coronavirus 229E (no rank) [taxon 11137], Cercopithecidae (monkey, family) [taxon 9527], Homo sapiens (human, species) [taxon 9606], Rattus norvegicus (brown rat, species) [taxon 10116], Human coronavirus NL63 (no rank) [taxon 277944]
- **Mutations:** E484Q, L452R
- **Cell lines:** Nl-63 — Homo sapiens (Human), Transformed cell line (CVCL_A8X2), NL-63 — Homo sapiens (Human), Induced pluripotent stem cell (CVCL_1E71)

## Full text

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## Figures

8 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12923118/full.md

## References

48 references — full list in the complete paper: https://tomesphere.com/paper/PMC12923118/full.md

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Source: https://tomesphere.com/paper/PMC12923118