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Developed by 
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Supported by 
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MK-8527
Developer(s)
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Merck Originator
https://www.merck.com/
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
MK-8527 Compound (4'-ethynyl-2-fluoro-2'-deoxyadenosine)
Drug information
Associated long-acting platforms
Oral solid form
Administration route
Oral
Therapeutic area(s)
Use case(s)
Use of drug
Ease of administration
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
Drug information
Drug's link(s)
Not provided
Generic name
Brand name
Compound type
Summary
Approval status
Regulatory authorities
Delivery device(s)
No delivery device
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.
Clinical trials
MK-8527-007
Identifier
NCT06045507
Link
https://clinicaltrials.gov/study/NCT06045507
Phase
Phase II
Status
Completed
Sponsor
Merck Sharp & Dohme LLC
More details
Not provided
Purpose
Evaluate the Safety, Tolerability, and Pharmacokinetics of Oral MK-8527 Once Monthly in Participants at Low-Risk for HIV-1 Infection.
Interventions
Intervention 1
Intervention 2
Countries
Sites / Institutions
Not provided
Trials dates
Anticipated Start Date
Not provided
Actual Start Date
2023-11-08
Anticipated Date of Last Follow-up
2025-03-11
Estimated Primary Completion Date
2025-02-18
Estimated Completion Date
2025-02-18
Actual Primary Completion Date
2024-12-12
Actual Completion Date
2025-02-12
Studied populations
Age Cohort
- Adults
- Older Adults
Genders
- All
Accepts pregnant individuals
No
Accepts lactating individuals
No
Accepts healthy individuals
Yes
Comments about the studied populations
Participants aged 18 to 65 years who are confirmed HIV-uninfected with low-risk of acquiring HIV. Participants are excluded if they have prior use of either islatravir (MK-8591) or MK-8527.
Health status
Study type
Interventional (clinical trial)
Enrollment
352
Allocation
Randomized
Intervention model
Parallel Assignment
Intervention model description
Not provided
Masking
Double-blind masking
Masking description
Double (Participant, Investigator)
Frequency of administration
Studied LA-formulation(s)
Studied route(s) of administration
Use case
PrEP
Key results
| Type of key results | Title | Website link |
|---|---|---|
| Article | South African National Clinical Trials Registry | https://sanctr.samrc.ac.za/TrialDisplay.aspx?TrialID=9389 |
MK-8527-002
Identifier
NCT03615183
Link
https://clinicaltrials.gov/study/NCT03615183
Phase
Phase I
Status
Completed
Sponsor
Merck Sharp & Dohme LLC
More details
Not provided
Purpose
Evaluate the Safety, Tolerability, Pharmacokinetics, and Anti-Retroviral Activity of MK-8527 Monotherapy in Anti-Retroviral Therapy (ART)-Naïve, HIV-1 Infected Participants.
Interventions
Intervention 1
Countries
Sites / Institutions
Not provided
Trials dates
Anticipated Start Date
Not provided
Actual Start Date
2019-02-11
Anticipated Date of Last Follow-up
2020-09-04
Estimated Primary Completion Date
Not provided
Estimated Completion Date
Not provided
Actual Primary Completion Date
2019-09-26
Actual Completion Date
2019-09-26
Studied populations
Age Cohort
- Adults
Genders
- All
Accepts pregnant individuals
No
Accepts lactating individuals
Unspecified
Accepts healthy individuals
No
Comments about the studied populations
Participants are ART-naïve HIV-1 positive individuals with a Body Mass Index (BMI) ≤35 kg/m^2, inclusive.
Health status
Study type
Interventional (clinical trial)
Enrollment
17
Allocation
Randomized
Intervention model
Sequential assignment
Intervention model description
Not provided
Masking
Open label
Masking description
None (Open Label)
Frequency of administration
Studied LA-formulation(s)
Studied route(s) of administration
Use case
Treatment
Key results
MK-8527-004
Identifier
NCT05494736
Link
https://clinicaltrials.gov/study/NCT05494736
Phase
Phase I
Status
Completed
Sponsor
Merck Sharp & Dohme LLC
More details
Activity of MK-8527 Monotherapy in Anti-Retroviral Therapy (ART)-Naïve, HIV-1 Infected Participants
Purpose
Evaluate the Safety, Tolerability, Pharmacokinetics, and Anti-Retroviral Activity of a Single Dose of MK-8527 Monotherapy in Anti-Retroviral Therapy (ART)-Naïve, HIV-1 Infected Participants.
Interventions
Intervention 1
Countries
Sites / Institutions
Not provided
Trials dates
Anticipated Start Date
Not provided
Actual Start Date
2022-11-17
Anticipated Date of Last Follow-up
2025-03-06
Estimated Primary Completion Date
Not provided
Estimated Completion Date
Not provided
Actual Primary Completion Date
2024-01-31
Actual Completion Date
2024-01-31
Studied populations
Age Cohort
- Adults
Genders
- All
Accepts pregnant individuals
No
Accepts lactating individuals
No
Accepts healthy individuals
No
Comments about the studied populations
Participants are ART-naïve HIV-1 positive individuals aged 18-60 years.
Health status
Study type
Interventional (clinical trial)
Enrollment
20
Allocation
Non-randomized
Intervention model
Sequential assignment
Intervention model description
Not provided
Masking
Open label
Masking description
None (Open Label)
Frequency of administration
Studied LA-formulation(s)
Studied route(s) of administration
Use case
Treatment
Key results
| Type of key results | Title | Website link |
|---|---|---|
| Article | AVAC trial entry | https://avac.org/trial/mk-8527-004/ |
MK-8527-008
Identifier
NCT06295796
Link
https://clinicaltrials.gov/study/NCT06295796
Phase
Phase I
Status
Completed
Sponsor
Merck Sharp & Dohme LLC
More details
The goal of this study is to evaluate the effect of moderate and severe renal impairment (RI) on the pharmacokinetics (PK), safety, and tolerability of MK-8527. There will be no hypothesis testing in the study.
Purpose
A Study of MK-8527 in Participants With Moderate and Severe Renal Impairment (MK-8527-008)
Interventions
Intervention 1
Countries
Sites / Institutions
Not provided
Trials dates
Anticipated Start Date
Not provided
Actual Start Date
2024-06-20
Anticipated Date of Last Follow-up
2025-02-05
Estimated Primary Completion Date
2024-03-06
Estimated Completion Date
2024-03-06
Actual Primary Completion Date
2025-01-31
Actual Completion Date
2025-01-31
Studied populations
Age Cohort
- Adults
- Older Adults
Genders
- All
Accepts pregnant individuals
Unspecified
Accepts lactating individuals
Unspecified
Accepts healthy individuals
Yes
Comments about the studied populations
Inclusion Criteria: The main inclusion criteria include but are not limited to the following: Moderate and Severe RI * With the exception of RI, is in sufficient health for study participation. * Has stable renal function. Healthy * Matches mean age to participants with moderate and severe RI. * Has normal renal function. Exclusion Criteria: The main exclusion criteria include but are not limited to the following: All participants * History of cancer (malignancy). * Positive test results for Human-immunodeficiency virus (HIV), Hepatitis B surface antigen (HBsAg), or Hepatitis C virus (HCV). * Had a major surgery or lost significant volume of blood within 56 days prior to dosing. * Donated plasma within 7 days prior to dosing. Moderate and Severe RI * Failed renal transplant or h
Health status
Not provided
Study type
Interventional (clinical trial)
Enrollment
18
Allocation
Non-randomized
Intervention model
Parallel Assignment
Intervention model description
Not provided
Masking
Open label
Masking description
Not provided
Frequency of administration
Studied LA-formulation(s)
Studied route(s) of administration
Use case
PrEP
Key results
MK-8527-012
Identifier
NCT06893081
Link
https://clinicaltrials.gov/study/NCT06893081
Phase
Phase I
Status
Not yet recruiting
Sponsor
Merck Sharp & Dohme LLC
More details
The goal of this study is to learn what happens to MK-8527 in a healthy person's body over time when MK-8527 is given alone and with the medication CBZ. Carbamazepine, sold under the brand name Tegretol among others, is an anticonvulsant medication used in the treatment of epilepsy and neuropathic pain. It is used as an adjunctive treatment in schizophrenia along with other medications and as a second-line agent in bipolar disorder.
Purpose
A Study of Carbamazepine (CBZ) and MK-8527 in Healthy Adult Participants (MK-8527-012)
Interventions
Intervention 1
Intervention 2
Countries
Not provided
Sites / Institutions
Not provided
Trials dates
Anticipated Start Date
2025-04-21
Actual Start Date
Not provided
Anticipated Date of Last Follow-up
2025-04-02
Estimated Primary Completion Date
2025-06-19
Estimated Completion Date
2025-06-19
Actual Primary Completion Date
Not provided
Actual Completion Date
Not provided
Studied populations
Age Cohort
- Adults
Genders
- All
Accepts pregnant individuals
No
Accepts lactating individuals
No
Accepts healthy individuals
Yes
Comments about the studied populations
Inclusion Criteria: Inclusion criteria include, but are not limited to: * Is a healthy, adult, male or female of non-childbearing potential only, 18-55 years of age, inclusive * Is a continuous non-smoker who has not used nicotine- and tobacco-containing products for at least 3 months prior Exclusion Criteria: Exclusion criteria include, but are not limited to: * Has a history or presence of: * Seizures (except for febrile seizure), or is at an increased risk for seizures * Family history of severe dermatologic reactions including toxic epidermal necrolysis and Stevens-Johnson syndrome * Clinically meaningful hematologic diseases, bone marrow disorders, or hematologic adverse reactions to other medications * Depression, unusual changes in mood or behavior or suicidal thoughts
Health status
Not provided
Study type
Interventional (clinical trial)
Enrollment
16
Allocation
Non-randomized
Intervention model
Single group assignment
Intervention model description
Not provided
Masking
Open label
Masking description
Not provided
Frequency of administration
Studied LA-formulation(s)
Studied route(s) of administration
Use case
PrEP
Key results
MK-8527-005
Identifier
EUCT2022-502081-24-00
Link
https://euclinicaltrials.eu/search-for-clinical-trials/?lang=en&EUCT=2022-502081-24-00
Phase
Phase I
Status
Completed
Sponsor
Merck Sharp & Dohme LLC
More details
A Multiple-Dose Clinical Study to Evaluate Safety, Tolerability, and Pharmacokinetics of MK-8527 in Healthy Participants
Purpose
A Multiple-Dose Clinical Study to Evaluate Safety, Tolerability, and Pharmacokinetics of MK-8527 in Healthy Participants
Interventions
Intervention 1
Countries
Sites / Institutions
Not provided
Trials dates
Anticipated Start Date
2022-12-07
Actual Start Date
Not provided
Anticipated Date of Last Follow-up
Not provided
Estimated Primary Completion Date
Not provided
Estimated Completion Date
2023-06-14
Actual Primary Completion Date
Not provided
Actual Completion Date
Not provided
Studied populations
Age Cohort
- Adults
- Older Adults
Genders
- Male
- Female
Accepts pregnant individuals
Unspecified
Accepts lactating individuals
Unspecified
Accepts healthy individuals
Yes
Comments about the studied populations
18-64 years
Health status
Study type
Interventional (clinical trial)
Enrollment
Not provided
Allocation
Non-randomized
Intervention model
Single group assignment
Intervention model description
Not provided
Masking
Open label
Masking description
Not provided
Frequency of administration
Studied LA-formulation(s)
Studied route(s) of administration
Use case
PrEP
Key results
MK-8527-013
Identifier
NCT06826989
Link
https://clinicaltrials.gov/study/NCT06826989
Phase
Phase I
Status
Recruiting
Sponsor
Merck Sharp & Dohme LLC
More details
The goal of this study is to learn how MK-8527 moves through a healthy person's body over time. Researchers will study how MK-8527 is absorbed by the body, broken down by the body, and how it leaves the body.
Purpose
A Study of MK-8527 in Healthy Adult Participants (PK PD) (MK-8527-013)
Interventions
Intervention 1
Countries
Sites / Institutions
Not provided
Trials dates
Anticipated Start Date
Not provided
Actual Start Date
2025-03-19
Anticipated Date of Last Follow-up
2025-04-07
Estimated Primary Completion Date
2025-05-07
Estimated Completion Date
2025-05-21
Actual Primary Completion Date
Not provided
Actual Completion Date
Not provided
Studied populations
Age Cohort
- Adults
Genders
- Male
Accepts pregnant individuals
No
Accepts lactating individuals
No
Accepts healthy individuals
Yes
Comments about the studied populations
Inclusion Criteria: * Is in good health * Has a body mass index (BMI) of 18 to 32 kg/m\^2 Exclusion Criteria: * Has a history of cancer * Has positive tests for hepatitis B surface antigen, hepatitis C antibodies or human immunodeficiency virus
Health status
Study type
Interventional (clinical trial)
Enrollment
8
Allocation
Non-randomized
Intervention model
Single group assignment
Intervention model description
Not provided
Masking
Open label
Masking description
Not provided
Frequency of administration
Studied LA-formulation(s)
Studied route(s) of administration
Use case
PrEP
Key results
MK-8527-009
Identifier
NCT06580587
Link
https://clinicaltrials.gov/study/NCT06580587
Phase
Phase I
Status
Recruiting
Sponsor
Merck Sharp & Dohme LLC
More details
The goal of this study is to learn how MK-8527 moves through the healthy person's body over time. Researchers will measure for the amount of MK-8527 in breast milk that the baby will receive at many time points.
Purpose
A Study of MK-8527 in Healthy Lactating Female Participants (MK-8527-009)
Interventions
Intervention 1
Countries
Sites / Institutions
Not provided
Trials dates
Anticipated Start Date
Not provided
Actual Start Date
2025-04-15
Anticipated Date of Last Follow-up
2025-04-21
Estimated Primary Completion Date
2025-12-19
Estimated Completion Date
2025-12-19
Actual Primary Completion Date
Not provided
Actual Completion Date
Not provided
Studied populations
Age Cohort
- Adults
- Older Adults
Genders
- Female
Accepts pregnant individuals
No
Accepts lactating individuals
Yes
Accepts healthy individuals
Yes
Comments about the studied populations
Inclusion Criteria: The key inclusion criteria include but are not limited to the following: * Is at least 6 weeks postpartum at the time of administration of study intervention, following the delivery of a healthy singleton neonate * Is willing and able to express breast milk at least twice daily for at least 120 hours after enrollment * Is willing to discontinue breastfeeding from the time of administration of study intervention until at least 6 weeks following the administration of study intervention. This includes the avoidance of both directly breastfeeding and the administration of breast milk pumped during the above-specified time frame to the infant. Is willing to confirm with the site that the infant is able to bottle feed (breast milk) prior to Day 1 and that alternative nutrit
Health status
Study type
Interventional (clinical trial)
Enrollment
12
Allocation
Not provided
Intervention model
Single group assignment
Intervention model description
Not provided
Masking
Open label
Masking description
Not provided
Frequency of administration
Studied LA-formulation(s)
Studied route(s) of administration
Use case
PrEP
Key results
MK-8527-006
Identifier
NCT06783192
Link
https://clinicaltrials.gov/study/NCT06783192
Phase
Phase I
Status
Completed
Sponsor
Merck Sharp & Dohme LLC
More details
This study is designed to assess the effect of a single dose of MK-8527 on the single-dose pharmacokinetics (PK) and the safety and tolerability of levonorgestrel/ethinyl estradiol (LNG/EE) in healthy adult postmenopausal or ovariectomized female participants.
Purpose
A Drug-Drug Interaction Study of MK 8527 With a Combined Oral Contraceptive (LNG/EE) in healthy adult postmenopausal or ovariectomized female participants.
Interventions
Intervention 1
Intervention 2
Countries
Sites / Institutions
Not provided
Trials dates
Anticipated Start Date
Not provided
Actual Start Date
2023-08-14
Anticipated Date of Last Follow-up
2025-01-14
Estimated Primary Completion Date
Not provided
Estimated Completion Date
Not provided
Actual Primary Completion Date
2023-10-11
Actual Completion Date
2023-10-11
Studied populations
Age Cohort
- Adults
- Older Adults
Genders
- Female
Accepts pregnant individuals
Unspecified
Accepts lactating individuals
Unspecified
Accepts healthy individuals
Yes
Comments about the studied populations
Inclusion Criteria: 18 Years to 70 Years (Adult, Older Adult ) * is in good overall health * assigned female at birth Exclusion Criteria: * has a history of clinically significant endocrine, GI, cardiovascular, hematological, thromboembolic, hepatic, immunological, renal, respiratory, genitourinary, or major neurological (including stroke and chronic seizures) abnormalities or diseases * is mentally or legally incapacitated, has significant emotional problems at the time of prestudy (screening) visit or expected during the conduct of the study or has a history of clinically significant psychiatric disorder of the last 5 years * has a history of cancer (malignancy)
Health status
Study type
Interventional (clinical trial)
Enrollment
14
Allocation
Non-randomized
Intervention model
Single group assignment
Intervention model description
Not provided
Masking
Open label
Masking description
Not provided
Frequency of administration
Studied LA-formulation(s)
Studied route(s) of administration
Use case
PrEP
Key results
| Type of key results | Title | Website link |
|---|---|---|
| Abstract | Phase 1, open-label study to evaluate the drug interaction between MK-8527, an HIV-1 nucleoside reverse transcriptase translocation inhibitor, and the oral contraceptive levonorgestrel/ethinyl estradi | https://www.natap.org/2024/IAS/IAS_115.htm |
8527-016
Identifier
NCT06816043
Link
https://clinicaltrials.gov/study/NCT06816043
Phase
Phase I
Status
Active, not recruiting
Sponsor
Merck Sharp & Dohme LLC
More details
The goal of this study is to learn what happens to MK-8527 in a healthy person's body over time, called a pharmacokinetic (PK) study. Researchers want to learn if there is a difference in the healthy person's body when MK-8527 is taken as a single dose (Treatment A) or with the medication Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF) (Treatment B).
Purpose
A Study of Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF) and MK-8527 in Healthy Participants
Interventions
Intervention 1
Intervention 2
Countries
Sites / Institutions
Not provided
Trials dates
Anticipated Start Date
Not provided
Actual Start Date
2025-02-21
Anticipated Date of Last Follow-up
2025-03-17
Estimated Primary Completion Date
2025-06-05
Estimated Completion Date
2025-06-05
Actual Primary Completion Date
Not provided
Actual Completion Date
Not provided
Studied populations
Age Cohort
- Adults
Genders
- All
Accepts pregnant individuals
Unspecified
Accepts lactating individuals
Unspecified
Accepts healthy individuals
Yes
Comments about the studied populations
Inclusion Criteria: The main inclusion criteria include but are not limited to the following: * Continuous non-smoker who has not used nicotine- and tobacco-containing products for at least 3 months prior * Has body mass index (BMI) ≥18 and ≤32.0 kg/m\^2 Exclusion Criteria: The main exclusion criteria include but are not limited to the following: * History of low bone density, renal impairment, Fanconi syndrome, autoimmune disorders (such as Graves' disease, polymyositis, Guillain-Barré syndrome, and autoimmune hepatitis), liver disease * History of cancer (malignancy) * Positive results for human immunodeficiency virus (HIV), hepatitis B surface antigen (HBsAg), or hepatitis C virus (HCV)
Health status
Study type
Interventional (clinical trial)
Enrollment
20
Allocation
Randomized
Intervention model
Cross-over assignment
Intervention model description
Not provided
Masking
Open label
Masking description
Not provided
Frequency of administration
Studied LA-formulation(s)
Studied route(s) of administration
Use case
PrEP
Key results
Excipients
Proprietary excipients used
Not provided
Novel excipients or existing excipients at a concentration above Inactive Ingredients Database (IID) for the specified route of administration
Not provided
Residual solvents used
Not provided
Patent info
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
Supporting material
Publications
There are no publication
Additional documents
No documents were uploaded
Access principles
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Collaborate for developmentConsider 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 Not provided |
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Share technical information for match-making assessmentProvide 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 Not provided |
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Work with MPP to expand access in LMICsIn 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 Not provided |
Comment & Information
Not provided