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Corporate presentation. (n.d.). https://www.cidara.com/wp-content/uploads/2023/09/Cidara-Corporate-Deck-September-2023.pdf
Based on public information

Technology name

Drug Fragment Conjugate (DFC)

Developer(s)

Sponsor(s)

Not specified

export_notes
Based on public information

Type of technology

Peptide of Human Antibody Fragment (Fc) coupled with drug molecule

Administration route

Subcutaneous, Intramuscular

Development state and regulatory approval

Active Pharmaceutical Ingredient (API)

Temsavir

Development Stage

Pre-clinical

Regulatory Approval

Not provided

Description

Drug Fc Conjugate is a long acting technology that acts as a single-molecule cocktail by coupling targeted small molecules and peptides to a human antibody fragment (Fc). These conjugates bind to the target receptors for an extended period while simultaneously engaging with the immune system of the human body, allowing them to both treat and prevent disease. DFC also has the potential to carry multiple targeting drug molecules.

Developer(s)

Cidara Therapeutics
United States of America

Cidara Therapeutics has developed a drug development pipeline platform called CloudBreak which is based on API conjugation with antibody fragment conjugate. This Drug Fc conjugate is a targeted immunotherapy that inhibits specific disease targets while simultaneously engaging the immune system. Cidara's portfolio includes novel therapeutics targeting viral infections and solid tumors.

Technology highlight

• Ability to target cryptic sites & has small molecule binding pockets • Targeted pharmacological action with low systematic exposure • Long half-life, similar to monoclonal antibody • Multivalent target engagement of DFC increases potency of API and reduces resistance potential • Extracellular targeted action

Illustration(s)

Technology main components

Drug -Fc Conjugate cocktail consists of (i) API, (ii) peptide fusions, and (iii) a human antibody fragment specific to the targeted disease (Fc MOIETY).

Information on the raw materials sourcing, availability and anticipated price

Not provided

Delivery device(s)

No delivery device

APIs compatibility profile

API desired features
Water-soluble molecules

Water-insoluble molecules

Small molecules

The DFC technology targets small molecules like Influenza neuroaminidase inhibitors (such as oseltamivir, zanamivir, peramivir, and laninamivir), CD73 inhibitors, CCR antagonists and GP120 inhibitors (such as temsavir).

Additional solubility data

Not provided

Additional stability data

Not provided

API loading: Maximum drug quantity to be loaded

Not provided

LogP

Not provided

Scale-up and manufacturing prospects

Scale-up prospects

WuXi XDC partnered with Cidara Therapeutics to manufacture DFC formulations. WuXi recently established a new manufacturing facility with the capacity to produce 200-2000 litres of DFC formulation per batch.

Tentative equipment list for manufacturing

Not provided

Manufacturing

Manufacturing of DFC formulation has low COGS.

Specific analytical instrument required for characterization of formulation

HPLC analytical procedure is used for the gross content and assay of reconstituted solution tests in the drug product specification

Excipients

Proprietary excipients used

No proprietary excipient used

Novel excipients or existing excipients at a concentration above Inactive Ingredient Database (IID) for the specified route of administration

No novel excipient or existing excipient used

Residual solvents used

No residual solvent used

Additional features

Other features of the technology
  • Drug-eluting
  • Other(s)

    Targeted action

Release properties

Small molecule conjugates in DFC exhibit selective targeting towards enzyme active sites and receptors. The distribution of the active pharmaceutical ingredient (API) is influenced by the molecular size of the DFC, with smaller sizes facilitating faster tissue penetration. The API is released from the Fc domain at the target site in a cumulative manner, optimizing therapeutic efficacy through sustained and controlled delivery for a longer period of time.

Injectability

Preclinical and clinical studies focused on DFC drug candidates administered via intramuscular (IM) and subcutaneous (SQ) routes. For administration, a 25-gauge or larger bore needle is used.

Safety

Interim analysis of Phase 2a studies of CD-388 shows that the drug was well-tolerated with no treatment emergent adverse events (TEAE) or serious adverse events (SAE) in 28 subjects who received CD-388.

Stability

Not provided

Storage conditions and cold-chain related features

The formulation should be stored at 20°C–25°C. It can also be stored at 5°C–25°C for up to 24 hours.

Therapeutic area(s)

  • Other(s) : "Influenza A & C infection"
  • Oncology
  • HIV
Use case(s)
  • Treatment

Potential associated API(s)

  • Temsavir

Use of technology

Ease of administration
  • Administered by a community health worker
  • Administered by a nurse
  • Administered by a specialty health worker
Frequency of administration

Weekly, Single dose administration

User acceptance

Not provided

Targeted user groups

Age Cohort
  • Adults
  • Older Adults
Genders
  • All
Pregnant individuals

No

Lactating individuals

No

Healthy individuals

Unspecified

Comment

Not provided

Temsavir

Class(es)

Antiretroviral

Development stage

Pre-clinical

Clinical trial number(s)

Not provided

Foreseen/approved indication(s)

HIV

Foreseen user group

Not provided

Foreseen duration between application(s)

Not provided

Applications to Stringent Regulatory Authorities (SRA) / regulatory approvals

Not provided

Description

Compositions and Methods for The Treatment of Viral Infections

Brief description

This patent pertains to antiviral drug conjugates and methods for inhibiting viral growth and treating viral infections that involves administering an effective amount of the conjugate, population of conjugates, or pharmaceutical composition to the subject. These conjugates contain monomers or dimers of a moiety that inhibit influenza virus neuraminidase, conjugated to Fc monomers, Fc domains, Fc-binding peptides, albumin proteins, or albumin protein-binding peptides. The neuraminidase inhibitor targets neuraminidase on the viral particle's surface, while the Fc domains bind to FcyRs on immune cells, activating phagocytosis and effector functions. These drug conjugates have enhanced antiviral activity.

Representative patent

WO2021046549A8

Category

treatment

Patent holder

Cidara Therapeutics, Inc

Exclusivity

Not provided

Expiration date

September 8, 2040

Status

Not provided

Description

Composition and Methods of treating Human Immunodeficiency Virus

Brief description

Conjugates containing viral gp120 receptor inhibitors (e.g., temsavir, BMS-818251, DMJ-ll-121, BNM-IV-147, or analogues thereof) linked to an Fc monomer, an Fc domain, an Fc-binding peptide, an albumin protein, or an albumin-binding peptide are used in the treatment of viral infections. These conjugates are particularly useful in the treatment of HIV infections.

Representative patent

WO2020252393A1

Category

Not provided

Patent holder

Cidara Therapeutics, Inc

Exclusivity

Not provided

Expiration date

June 12, 2040

Status

Not provided

Description

Compositions and Methods for the Treatment of Bacterial infections

Brief description

Conjugates with an Fc domain covalently bonded to one or more monomers or dimers of cyclic heptapeptides are among the compositions and methods used to treat bacterial infections. These small-molecule conjugates have the potential to treat gram-negative bacterial infections.

Representative patent

US20230190950A1

Category

Not provided

Patent holder

Cidara Therapeutics, Inc

Exclusivity

Not provided

Expiration date

December 20, 2037

Status

Not provided

Publications

There are no publication

Collaborate for development

Consider on a case by case basis, collaborating on developing long acting products with potential significant public health impact, especially for low- and middle-income countries (LMICs), utilising the referred to long-acting technology

Share technical information for match-making assessment

Provide necessary technical information to a potential partner, under confidentiality agreement, to enable preliminary assessment of whether specific medicines of public health importance in LMICs might be compatible with the referred to long-acting technology to achieve a public health benefit

Work with MPP to expand access in LMICs

In the event that a product using the referred to long-acting technology is successfully developed, the technology IP holder(s) will work with the Medicines Patent Pool towards putting in place the most appropriate strategy for timely and affordable access in low and middle-income countries, including through licensing

All sponsors

No sponsor indicated

Comment & Information