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Drug information

Drug's link(s)

Not provided

Generic name

MK-8527

Brand names

investigational

Compound type

Small molecule

Summary

MK-8527 is a nucleoside reverse transcriptase translocation inhibitor (NRTTI) currently in clinical development for the prevention of HIV-1. It is similar to islatravir. MK-8527 is a 7-deaza-deoxyadenosine analog and is phosphorylated intracellularly to its active triphosphate (TP) form, which is a potent inhibitor of HIV-1 replication. MK-8527 functions by preventing the translocation of the HIV reverse transcriptase enzyme, thereby disrupting viral replication. Ongoing trials are assessing MK-8257 as a once-monthly oral PrEP otpion.

Approval status

MK-8527 is currently in clinical development and not yet approved in any jurisdiction.

Regulatory authorities

MK-8527 is currently in clinical development and not yet approved in any jurisdiction.

Therapeutic area(s)

  • HIV
Use case(s)
  • Pre-Exposure Prophylaxis (PrEP)
  • Prevention

Administration route

Oral

Associated long-acting platforms

Oral solid form

Use of drug

Ease of administration
  • Self-administered
User acceptance

A monthly oral PrEP option would probably fit well in many settings and be convenient for a number of clients. This will be further investigated.

Dosage

Available dose and strength

Doses of 0.25 mg, 0.5mg, 1mg, 3mg, 10 mg and 12 mg are being evaluated in clinical programs.

Frequency of administration

Investigated for once monthly oral dosing for HIV PrEP

Maximum dose

Doses of 0.25 mg, 0.5mg, 1mg, 3mg and 10 mg are being evaluated in clinical programs.

Recommended dosing regimen

Doses of 0.25 mg, 0.5mg, 1mg, 3mg and 10 mg are being evaluated in clinical programs as once monthly oral dosing

Additional comments

MK-8527 is on the priority list of MPP since March 2025, as a candidate for which voluntary licensing and technology transfer through MPP would lead to expanded access, significant health benefits, and substantial public health impact compared to available standards of care (https://medicinespatentpool.org/progress-achievements/prioritisation#pills-hiv)

Dosage link(s)

Not provided

Associated technologies

Not provided

Comment & Information

Not provided

Developer(s)

Merck
Originator
United States

Merck & Co., Inc. is an American multinational pharmaceutical company known as Merck Sharp & Drone (MSD) in territories outside of the USA and Canada. Merck was originally established in 1891, and is currently headquartered in Rahway, New Jersey. The company is particularly well known for developing and manufacturing biologic therapies, vaccines, medicines and animal health products.

Drug structure

Scale-up and manufacturing prospects

Scale-up prospects

Detailed manufacturing information is not currently available for this compound.

Tentative equipment list for manufacturing

Detailed manufacturing information is not currently available for this compound.

Manufacturing

Detailed manufacturing information is not currently available for this compound.

Specific analytical instrument required for characterization of formulation

Detailed manufacturing information is not currently available for this compound.

Excipients

Proprietary excipients used

Not provided

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

Not provided

Residual solvents used

Not provided

Delivery device(s)

No delivery device

Description

4'-SUBSTITUTED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS

Brief description

4'-substituted nucleoside derivatives of Formula I and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC.

Representative patent

WO2015143712

Category

Compound

Patent holder

Merck Sharp & Dohme Corp.

Exclusivity

Not provided

Expiration date

March 28, 2034

Status

Granted in 36 countries: AL, AM, AP (BW, GH, KE, NA), AT, AU, AZ, BA, BE, BG, BY, CA, CH, CL, CN, CR, CY, CZ, DE, DK, DZ, EA, EE, ES, FI, FR, GB, GC, GE, GI, GR, GY, HN, HR, HU, ID, IE, IL, IR, IS, IT, JO, JP, KR, KZ, LB, LT, LU, LV, MA, ME, MK, MN, MT, MX, MY, NG, NL, NO, NZ, PA, PE, PH, PK, PL, PT, RO, RS, RU, SC, SE, SG, SI, SK, TN, TR, TT, TW, UA, US, VE, VN, ZA Filed in 13 countries: AR, BB, BN, BR, BZ, DO, EC, EG, GT, IN, JM, LK, NI, SV, TH As of 27 June 2024 - MPP Search

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