Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Label indication Adult Patients: ISENTRESS and ISENTRESS HD are human immunodeficiency virus integrase strand transfer inhibitors (HIV- FDA label
Also known as MK0518 (Raltegravir), raltegravir, Isentress®
MK0518 · 13 trials · 7 indications
Incidence of acute clinical renal graft rejection defined by 20% increase of serum creatinine, associated to histological features (Banff classification) 6 months after renal transplantation
Numbers of participants with HIV RNA copies \<50 copies/mL were summarized by race for each time point.
Numbers of participants with one or more adverse events were summarized by race.
Numbers of participants who discontinued due to an adverse event were summarized by race.
Antiretroviral activity was evaluated for participants who achieved HIV RNA level \<50 copies/mL at Week 48.
An adverse experience (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study drug, whether or not considered related to the use of the product.
Serious CAEs are any AEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose.
Adverse experiences (AEs) in this study were defined as "drug-related" if the investigator, who is a qualified physician, considered the AE as possibly, probably, or definitely related to MK-0518 or efavirenz alone or in combination with TRUVADA® or to TRUVADA® alone according to his/her best clinical judgment.
Serious CAEs are any AEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose. Adverse experiences (AEs) in this study were defined as "drug-related" if the investigator, who is a qualified physician, considered the AE as possibly, probably, or definitely related to MK-0518 or efavirenz alone or in combination with TRUVADA® or to TRUVADA® alone according to his/her best clinical judgment.
All participant deaths in the span of 48 weeks on study were recorded.
An adverse experience (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study drug, whether or not considered related to the use of the product.
Serious CAEs are any AEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose.
Adverse experiences (AEs) in this study were defined as "drug-related" if the investigator, who is a qualified physician, considered the AE as possibly, probably, or definitely related to MK-0518 or efavirenz alone or in combination with TRUVADA® or to TRUVADA® alone according to his/her best clinical judgment.
Serious CAEs are any AEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose. Adverse experiences (AEs) in this study were defined as "drug-related" if the investigator, who is a qualified physician, considered the AE as possibly, probably, or definitely related to MK-0518 or efavirenz alone or in combination with TRUVADA® or to TRUVADA® alone according to his/her best clinical judgment.
A laboratory AE is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the study product, whether or not considered related to the use of the product.
A laboratory AE is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the study product, whether or not considered related to the use of the product. Serious AEs are any AEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose.
A laboratory AE is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the study product, whether or not considered related to the use of the product. Adverse experiences (AEs) in this study were defined as "drug-related" if the investigator, who is a qualified physician, considered the AE as possibly, probably, or definitely related to MK-0518 or efavirenz alone or in combination with TRUVADA® or to TRUVADA® alone according to his/her best clinical judgment.
A laboratory AE is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the study product, whether or not considered related to the use of the product. Serious AEs are any AEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose. Adverse experiences (AEs) in this study were defined as "drug-related" if the investigator, who is a qualified physician, considered the AE as possibly, probably, or definitely related to MK-0518 or efavirenz alone or in combination with TRUVADA® or to TRUVADA® alone according to his/her best clinical judgment.
A laboratory AE is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the study product, whether or not considered related to the use of the product.
A laboratory AE is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the study product, whether or not considered related to the use of the product. Adverse events (AEs) in this study were defined as "drug-related" if the investigator considered the AE as possibly, probably, or definitely related to MK-0518 or efavirenz alone or in combination with TRUVADA® or to TRUVADA® alone.
Percentage of participants who achieved HIV RNA \<400 copies/mL at Week 16
Percentage of participants who achieved HIV RNA \<400 copies/mL at Week 48
Percentage of participants who achieved HIV RNA \<400 copies/mL at Week 156
Percentage of participants who achieved HIV RNA \<400 Copies/mL at Week 240
Mean changes in alkaline phosphatase levels after 12 months treatment with combination antiretroviral therapy or placebo.
Mean change from baseline at Week 24 in HIV RNA (log10 copies/mL) in all patients
Mean change from baseline on Day 10 in plasma Human Immunodeficiency Virus (HIV) Ribonucleic acid (RNA) (copies/mL)
An adverse experience (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the SPONSOR'S product, whether or not considered related to the use of the product. Serious CAEs are any AEs occurring at any dose that; Results in death; or Is life threatening; or Results in a persistent or significant disability/incapacity; or Results in or prolongs an existing inpatient hospitalization; or Is a congenital anomaly/birth defect; or Is a cancer; or Is an overdose.
An adverse experience (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the SPONSOR'S product, whether or not considered related to the use of the product.
Serious CAEs are any AEs occurring at any dose that; Results in death; or Is life threatening; or Results in a persistent or significant disability/incapacity; or Results in or prolongs an existing inpatient hospitalization; or Is a congenital anomaly/birth defect; or Is a cancer; or Is an overdose
An adverse experience (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the SPONSOR'S product, whether or not considered related to the use of the product An adverse experience (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the SPONSOR'S product, whether or not considered related to the use of the product
An AE was defined as any unfavorable \& unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study drug, whether or not considered related to its use. Any worsening of a preexisting condition which was temporally associated with the use of the study drug, was also an AE. A SAE was any AE that resulted in death, was life threatening, resulted in a persistent or significant disability/incapacity, resulted in or prolonged an existing inpatient hospitalization, was a congenital anomaly/birth defect, was cancer, or was an overdose.
HIV RNA levels were determined by AMPLICOR HIV-1 Monitor™ UltraSensitive Assay.
In Period 1 participants were treated with 1200 mg raltegravir alone; followed by Period 2 where participants were treated with 1200 mg raltegravir and three tablets of TUMS Ultra Strength (US) 1000 taken orally concomitantly; followed by Period 3 where participants were treated with 1200 mg raltegravir and 12 hours later with 20 mL Leader Antacid Maximum Strength (MS) taken orally; followed by Period 4 where participants were treated with 1200 mg raltegravir and 12 hours later with three tablets of TUMS US 1000 taken orally. The wait between Periods was a maximum of 7 days, during which participants were treated with 1200 mg raltegravir once daily. To determine the plasma concentration of raltegravir, blood samples were collected from pre-dose up to 24 hours post-dose, and analysis of variance (ANOVA) modeling was performed on natural log-transformed values to derive geometric least-squares means.
In Period 1 participants were treated with 1200 mg raltegravir alone; followed by Period 2 where participants were treated with 1200 mg raltegravir and three tablets of TUMS US 1000 taken orally concomitantly; followed by Period 3 where participants were treated with 1200 mg raltegravir and 12 hours later with 20 mL Leader Antacid MS taken orally; followed by Period 4 where participants were treated with 1200 mg raltegravir and 12 hours later with three tablets of TUMS US 1000 taken orally. The wait between Periods was a maximum of 7 days, during which participants were treated with 1200 mg raltegravir once daily. To determine the plasma concentration of raltegravir, blood samples were collected from pre-dose up to 24 hours post-dose, and ANOVA modeling was performed on natural log-transformed values to derive geometric least-squares means.
In Period 1 participants were treated with 1200 mg raltegravir alone; followed by Period 2 where participants were treated with 1200 mg raltegravir and three tablets of TUMS US 1000 taken orally concomitantly; followed by Period 3 where participants were treated with 1200 mg raltegravir and 12 hours later with 20 mL Leader Antacid MS taken orally; followed by Period 4 where participants were treated with 1200 mg raltegravir and 12 hours later with three tablets of TUMS US 1000 taken orally. The wait between Periods was a maximum of 7 days, during which participants were treated with 1200 mg raltegravir once daily. To determine the plasma concentration of raltegravir, blood samples were collected at 24 hours post-dose, and ANOVA modeling was performed on natural log-transformed values to derive geometric least-squares means.
Blood was drawn 12 hours after dosing with raltegravir in order to determine the geometric mean plasma concentration.
Blood was drawn at time 0, and at various intervals up to 12 hours after dosing with raltegravir in order to determine the geometric mean area under the curve plasma concentration versus time.
Blood was drawn at time 0, and at various intervals up to 12 hours after dosing with raltegravir, in order to determine the geometric mean maximum plasma concentration.
Blood was drawn 12 hours after dosing with raltegravir in order to determine the geometric mean plasma concentration.
Blood was drawn at time 0, and at various intervals up to 12 hours after dosing with raltegravir, in order to determine the geometric mean area under the curve plasma concentration versus time.
Blood was drawn at time 0, and at various intervals up to 12 hours after dosing with raltegravir, in order to determine the geometric mean maximum plasma concentration.
Participant blood samples were collected to measure the steady state plasma concentration of raltegravir 12 hours after administration alone or with a single dose of antacid. The primary hypothesis compared C12hrs of raltegravir when administered alone with C12hrs of raltegravir when coadministered with TUMS® or MINTOX®.
Participant blood samples were collected to measure the steady state plasma concentration of raltegravir 12 hours after administration alone or before or after a single dose of antacid. The secondary hypothesis compared C12hrs of raltegravir when administered alone with C12hrs of raltegravir when administered 2 hours before or after MINTOX®.
Participant blood samples were collected to measure the steady state AUC of raltegravir up to 12 hours after administration alone or with a single dose of antacid. The primary hypothesis compared AUC0-12hrs of raltegravir when administered alone with AUC0-12hrs of raltegravir when coadministered with TUMS® or MINTOX®.
Participant blood samples were collected to measure the steady state AUC of raltegravir up to 12 hours after administration alone or before or after a single dose of antacid. The secondary hypothesis compared AUC0-12hrs of raltegravir when administered alone with AUC0-12hrs of raltegravir when administered 2 hours before or after MINTOX®.
Participant blood samples were collected to measure the steady state maximum plasma concentration of raltegravir when administered alone or with a single dose of antacid. The primary hypothesis compared Cmax of raltegravir when administered alone with Cmax of raltegravir when coadministered with TUMS® or MINTOX®.
Participant blood samples were collected to measure the maximum steady state plasma concentration of raltegravir after administration alone or before or after a single dose of antiacid. The secondary hypothesis compared Cmax of raltegravir when administered alone with Cmax of raltegravir when administered 2 hours before or after MINTOX®.
Participant blood samples were collected to measure the time to achieve the maximum steady state plasma concentration of raltegravir when administered alone or with a single dose of antacid
An AE is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study drug, whether or not considered related to the use of the product. Any worsening of a preexisting condition which is temporally associated with the use of the study drug is also an adverse experience.
Area Under the Plasma Concentration-Time Curve and peak concentration
| Arm | Type | Description |
|---|---|---|
| Raltegravir | EXPERIMENTAL | Raltegravir associated to an antiretroviral regimen without ritonavir boosted antiprotease |
| 1 | EXPERIMENTAL | raltegravir |
| MK-0518 400 mg b.i.d. | EXPERIMENTAL | MK-0518 400 mg, which can be taken by mouth (PO) twice a day (b.i.d.) without regard to food, and placebo to efavirenz, which will be taken PO at bedtime (q.h.s.) on an empty stomach preferably at bedtime. All participants will take one tablet of TRUVADA® (200 mg of emtricitabine and 300 mg of tenofovir disoproxil fumarate) with food, daily with the morning dose of MK-0518. Dosing interval adjustment of TRUVADA® is recommended in all participants with creatinine clearance 30-49 mL/min. |
| Efavirenz 600 mg q.h.s. | ACTIVE_COMPARATOR | Efavirenz 600 mg, which will be taken by mouth (PO) at bedtime (q.h.s.) on an empty stomach preferably at bedtime, and placebo to MK-0518, which will be taken PO twice a day (b.i.d.) without regard to food. All participants will take one tablet of TRUVADA® with food, daily with the morning dose of placebo. Dosing interval adjustment of TRUVADA® is recommended in all participants with creatinine clearance 30-49 mL/min. |
| 2 | PLACEBO_COMPARATOR | Placebo |
| Emtricitabine (FTC)/Tenofovir Disoproxil (TDF) & Raltegravir | EXPERIMENTAL | one Emtricitabine 200mg and Tenofovir Disoproxil 300mg tablet two Raltegravir 600mg tablets |
| Placebo | PLACEBO_COMPARATOR | Identical tablets resembling one Emtricitabine 200mg and Tenofovir Disoproxil 300mg tablet two Raltegravir 600mg tablets |
| 3 | EXPERIMENTAL | MK0518 600 mg |
| 4 | PLACEBO_COMPARATOR | Placebo |
| 600 mg monotherapy | EXPERIMENTAL | MK0518 600 mg twice daily |
| 400 mg monotherapy | EXPERIMENTAL | MK0518 400 mg twice daily |
| 200 mg monotherapy | EXPERIMENTAL | MK0518 200 mg twice daily |
| 100 mg monotherapy | EXPERIMENTAL | MK0518 100 mg twice daily |
| placebo monotherapy | PLACEBO_COMPARATOR | Placebo to MK0518 twice daily |
| 600 mg combo therapy | EXPERIMENTAL | MK0518 600 mg + tenofovir + lamivudine |
| 400 mg combo therapy | EXPERIMENTAL | MK0518 400 mg + tenofovir + lamivudine |
| 200 mg combo therapy | EXPERIMENTAL | MK0518 200 mg + tenofovir + lamivudine |
| 100 mg combo therapy | EXPERIMENTAL | MK0518 100 mg + tenofovir + lamivudine |
| EFV combo therapy | ACTIVE_COMPARATOR | efavirenz + tenofovir + lamivudine |
| 001 | EXPERIMENTAL | TMC278 One 25 mg tablet once daily for 11 days (TrtA and C) |
| 002 | EXPERIMENTAL | Raltegravir One 400 mg tablet twice daily for 4 days (Trt B) and for 11 days (TrtC) |
| Raltegravir Pre- and 4 Period Sequence | EXPERIMENTAL | Starting five days prior to Period 1 participants will be treated with 1200 mg raltegravir, once daily for five days. In Period 1 participants will be treated with 1200 raltegravir alone; this is followed by Period 2 where participants will be treated with 1200 mg raltegravir and TUMS concomitantly; this is followed by Period 3 where participants will be treated with 1200 mg raltegravir and 12 hours later with Leader Antacid; followed by Period 4 where participants will be treated with 1200 mg raltegravir and 12 hours later with TUMS. The wait between Periods is 2-7 days. |
| Ralt→MAL4Ralt→Ralt4MAL→MAL6Ralt→Ralt6MAL | EXPERIMENTAL | Part 1 was comprised of periods 1, 2 and 3; Part 2 was comprised of periods 4 and 5; with each study period separated by a washout period of at least 2 days. Part 1 was separated from Part 2 by a Pause. Each period had single oral dose treatments as follows: Raltegravir (Ralt) alone in Period 1, MAALOX (MAL) followed 4 hrs later by Ralt in Period 2, Ralt followed 4 hrs later by MAL in Period 3, MAL followed 6 hrs later by Ralt in Period 4, Ralt followed 6 hrs later by MAL in Period 5 |
| MAL4Ralt→Ralt4MAL→Ralt→MAL6Ralt→Ralt6MAL | EXPERIMENTAL | Part 1 was comprised of periods 1, 2 and 3; Part 2 was comprised of periods 4 and 5; with each study period separated by a washout period of at least 2 days. Part 1 was separated from Part 2 by a Pause. Each period had single oral dose treatments as follows: MAL followed 4 hrs later by Ralt in Period 1, Ralt followed 4 hrs later by MAL in Period 2, Ralt alone in Period 3, MAL followed 6 hrs later by Ralt in Period 4, Ralt followed 6 hrs later by MAL in Period 5 |
| Ralt4MAL→Ralt→MAL4Ralt→MAL6Ralt→Ralt6MAL | EXPERIMENTAL | Part 1 was comprised of periods 1, 2 and 3; Part 2 was comprised of periods 4 and 5; with each study period separated by a washout period of at least 2 days. Part 1 was separated from Part 2 by a Pause. Each period had single oral dose treatments as follows: Ralt followed 4 hrs later by MAL in Period 1, Ralt alone in Period 2, MAL followed 4 hrs later by Ralt in Period 3, MAL followed 6 hrs later by Ralt in Period 4, Ralt followed 6 hrs later by MAL in Period 5 |
| Ralt→Ralt4MAL→MAL4Ralt→Ralt6MAL→MAL6Ralt | EXPERIMENTAL | Part 1 was comprised of periods 1, 2 and 3; Part 2 was comprised of periods 4 and 5; with each study period separated by a washout period of at least 2 days. Part 1 was separated from Part 2 by a Pause. Each period had single oral dose treatments as follows: Ralt alone in Period 1, Ralt followed 4 hrs later by MAL in Period 2, MAL followed 4 hrs later by Ralt in Period 3, Ralt followed 6 hrs later by MAL in Period 4, MAL followed 6 hrs later by Ralt in Period 5 |
| MAL4Ralt→Ralt→Ralt4MAL→Ralt6MAL→MAL6Ralt | EXPERIMENTAL | Part 1 was comprised of periods 1, 2 and 3; Part 2 was comprised of periods 4 and 5; with each study period separated by a washout period of at least 2 days. Part 1 was separated from Part 2 by a Pause. Each period had single oral dose treatments as follows: MAL followed 4 hrs later by Ralt in Period 1, Ralt alone in Period 2, Ralt followed 4 hrs later by MAL in Period 3, Ralt followed 6 hrs later by MAL in Period 4, MAL followed 6 hrs later by Ralt in Period 5 |
| Ralt4MAL→MAL4Ralt→Ralt→Ralt6MAL→MAL6Ralt | EXPERIMENTAL | Part 1 was comprised of periods 1, 2 and 3; Part 2 was comprised of periods 4 and 5; with each study period separated by a washout period of at least 2 days. Part 1 was separated from Part 2 by a Pause. Each period had single oral dose treatments as follows: Ralt followed 4 hrs later by MAL in Period 1, MAL followed 4 hrs later by Ralt in Period 2, Ralt alone in Period 3, Ralt followed 6 hrs later by MAL in Period 4, MAL followed 6 hrs later by Ralt in Period 5 |
| RAL, TUMS+RAL, MINTOX+RAL, MINTOX Before RAL, MINTOX After RAL | EXPERIMENTAL | Participants received Raltegravir in treatment period 1, followed by TUMS® + Raltegravir in treatment period 2, followed by MINTOX® + Raltegravir in treatment period 3, followed by MINTOX® 2 hours before Raltegravir in treatment period 4, followed by MINTOX® 2 hours After Raltegravir in treatment period 5. There was a 2-day washout between treatment periods. |
| TUMS+RAL, MINTOX+RAL, RAL, MINTOX Before RAL, MINTOX After RAL | EXPERIMENTAL | Participants received TUMS® + Raltegravir in treatment period 1, followed by MINTOX® + Raltegravir in treatment period 2, followed by Raltegravir in treatment period 3, followed by MINTOX® 2 hours before Raltegravir in treatment period 4, followed by MINTOX® 2 hours after Raltegravir in treatment period 5. There was a minimum 2-day washout between treatment periods. |
| MINTOX+RAL, RAL, TUMS+RAL, MINTOX Before RAL, MINTOX After RAL | EXPERIMENTAL | Participants received MINTOX® + Raltegravir in treatment period 1, followed by Raltegravir in treatment period 2, followed by TUMS® + Raltegravir in treatment period 3, followed by MINTOX® 2 hours before Raltegravir in treatment period 4, followed by MINTOX® 2 hours after Raltegravir in treatment period 5. There was a minimum 2-day washout between treatment periods. |
| RAL, MINTOX+RAL, TUMS+RAL, MINTOX After RAL, MINTOX Before RAL | EXPERIMENTAL | Participants received Raltegravir in treatment period 1, followed by MINTOX® + Raltegravir in treatment period 2, followed by TUMS® + Raltegravir in treatment period 3, followed by MINTOX® 2 hours after Raltegravir in treatment period 4, followed by MINTOX® 2 hours before Raltegravir in treatment period 5. There was a minimum 2-day washout between treatment periods. |
| TUMS+RAL, RAL, MINTOX+RAL, MINTOX After RAL, MINTOX Before RAL | EXPERIMENTAL | Participants received TUMS® + Raltegravir in treatment period 1, followed by Raltegravir in treatment period 2, followed by MINTOX® + Raltegravir in treatment period 3, followed by MINTOX® 2 hours after Raltegravir in treatment period 4, followed by MINTOX® 2 hours before Raltegravir in treatment period 5. There was a minimum 2-day washout between treatment periods. |
| MINTOX+RAL, TUMS+RAL, RAL, MINTOX After RAL, MINTOX Before RAL | EXPERIMENTAL | Participants received MINTOX® + Raltegravir in treatment period 1, followed by TUMS® + Raltegravir in treatment period 2, followed by Raltegravir in treatment period 3, followed by MINTOX® 2 hours after Raltegravir in treatment period 4, followed by MINTOX® 2 hours before Raltegravir in treatment period 5. There was a minimum 2-day washout between treatment periods. |
| Period 1 | EXPERIMENTAL | MK0518 |
| Period 2 | EXPERIMENTAL | famotidine + MK0518 |
| Period 3 | EXPERIMENTAL | omeprazole + MK0518 |
| Name | Type | Description |
|---|---|---|
| Raltegravir | DRUG | Introduction of Raltegravir 2 days after renal transplantation within an antiretroviral regimen without ritonavir boosted antiprotease |
| Comparator: raltegravir | DRUG | 400 mg tablets taken twice daily. Total treatment period is 48 weeks. |
| MK-0518 | DRUG | 400 mg MK-0518 tablet taken by mouth (PO) twice a day (b.i.d.) for up to 240 weeks |
| Comparator: efavirenz | DRUG | 600 mg efavirenz tablet taken by mouth (PO) every night (q.h.s.) for up to 240 weeks |
| Comparator: Truvada | DRUG | One tablet Truvada once a day (q.d.) for up to 240 weeks (one tablet contains 200 mg emtricitabine and 300 mg tenofovir) |
| Comparator: Placebo to MK-0518 | DRUG | Placebo to MK-0518 PO b.i.d., taken for up to 240 weeks |
| Comparator: Placebo to efavirenz | DRUG | Placebo to efavirenz PO every night (q.h.s.), taken for up to 240 weeks |
| raltegravir potassium | DRUG | Raltegravir 400 mg twice daily (b.i.d.) by mouth (p.o.) with optimized background therapy. Treatment period of 48 weeks. |
| Comparator: placebo | DRUG | Placebo p.o. b.i.d. with optimized background therapy. Treatment period of 48 weeks. |
| Emtricitabine (FTC)/Tenofovir Disoproxil (TDF) | DRUG | Emtricitabine (FTC) 200 mg/Tenofovir Disoproxil (TDF) 300 mg by mouth once per day |
| Placebo Oral Capsule [CEBOCAP] | DRUG | Two capsules identical to Raltegravir and one capsule identical to Truvada with no active ingredients by mouth once per day |
| Comparator: MK0518 | DRUG | MK0518 oral tablets 200 mg b.i.d, for 24 weeks |
| MK0518 | DRUG | MK0518 oral tablets 400 mg b.i.d, for 24 weeks |
| Placebo | DRUG | Placebo to MK0518, oral tablet b.i.d, for 24 weeks |
| Comparator: MK0518 monotherapy | DRUG | MK0518 twice daily for 10 days |
| Comparator: MK0518 combination therapy | DRUG | MK0518 twice daily for 48 weeks |
| Comparator: tenofovir | DRUG | tenofovir 300 mg daily for 48 weeks |
| Comparator: lamivudine | DRUG | lamivudine 300 mg daily for 48 weeks |
| Placebo monotherapy | DRUG | Placebo to MK0518 twice daily |
| TMC278 | DRUG | One 25 mg tablet, once daily, for 11 days (TrtA and C) |
| Raltegravir 1200 mg | DRUG | Two tablets of 600 mg raltegravir administered orally, once daily, over 5 days of Pre-treatment, and once at the start of Periods 1-4. |
| TUMS | DRUG | Three tablets of TUMS Ultra Strength (US) 1000, taken orally, concomitantly with raltegravir in Period 2, and 12 hours after raltegravir in Period 4 |
| Leader Antacid | DRUG | 20 mL Leader Antacid Maximum Strength (MS) taken orally 12 hours after raltegravir, in Period 3 |
| Raltegravir (ISENTRESS™) | DRUG | Raltegravir 400 mg oral tablet once every 12 hours. Participants will continue with their other prescribed antiretroviral agents throughout the study. |
| MAALOX (MAL) | DRUG | MAL (or generic equivalent) 20 mL oral single dose on Day 1 |
| TUMS® Ultra Strength | DRUG | 3 tablets TUMS® Ultra Strength (US) 1000 mg Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days washout between treatment periods. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. |
| MINTOX® Maximum Strength | DRUG | 20 mL MINTOX® Maximum Strength (MS) Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days washout between treatment periods. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. |
| MK0518 (Raltegravir) | DRUG | 400 mg oral tablet of MK0518 once every 12 hours. Period 1 duration is one day, Period 2 duration is one day, Period 3 duration is five days. |
| famotidine | DRUG | Single 20 mg famotidine oral tablet taken 2 hours prior to administration of AM dose of MK0518 |
| omeprazole | DRUG | 20 mg oral tablet of omeprazole, once daily for 5 days |
Inclusion Criteria: * Registration on the French national renal transplantation waiting list (Biomedicines Agency) for a living or cadaveric donor organ * HIV-1-infected patients treated by a three-drug ARV regimen * Immuno-virologic criteria at renal transplantation: undetectable viral load (\<50 ...
Top 19 of 30 competitors
| Company | Ticker | Trials | Lead Phase | Drugs |
|---|---|---|---|---|
| Pfizer Inc. | PFE | 7 | PHASE3 | VLA15, Prevenar 20, 13vPnC, ATM-AVI, PG4 |
| Sanofi SA Sponsored ADR | SNY | 1 | PHASE3 | PCV21 |
| GSK plc Sponsored ADR | GSK | 4 | PHASE2 | Penmenvy, iNTS-TCV, Strep A vaccine, Pan-Salmonella vaccine |
| Grifols, S.A. Sponsored ADR Class B | GRFS | 1 | PHASE3 | Xembify |
| CorMedix Inc. | CRMD | 1 | PHASE3 | DefenCath |
| Sinovac Biotech Ltd. | SVA | 4 | PHASE3 | Sinovac PCV24, Group ACYW135X Meningococcal Conjugate Vaccine, Group ACYW135 Meningococcal Conjugate Vaccine |
| Novartis AG Sponsored ADR | NVS | 2 | PHASE2 | EDI048 |
| Innoviva, Inc. | INVA | 3 | PHASE2 | Eravacycline, Sulbactam-durlobactam |
| BiomX Inc. | PHGE | 1 | PHASE2 | BX004 |
| Hoffmann-La Roche | RHHBY | 1 | PHASE3 | Baloxavir Marboxil |
| Merck & Co., Inc. | MRK | 2 | PHASE1 | V118C |
| AstraZeneca PLC | AZN | 1 | PHASE1 | AZD7760 |
| BioNTech SE Sponsored ADR | BNTX | 1 | PHASE1 | BNT163 |
| 60 Degrees Pharmaceuticals, Inc. | SXTP | 1 | PHASE2 | Tafenoquine |
| Tarsus Pharmaceuticals, Inc. | TARS | 1 | PHASE2 | TP-05 |
| Moderna, Inc. | MRNA | 1 | PHASE2 | mRNA-1982 |
| AN2 Therapeutics, Inc. | ANTX | 1 | PHASE2 | Epetraborole |
| Emergent BioSolutions Inc. | EBS | 4 | - | AIGIV/kg |
| Phathom Pharmaceuticals, Inc. | PHAT | 1 | - | Vonoprazan |
MK0518 is used to treat HIV infections, including HIV-1 infection. It has been studied in treatment-naive HIV-infected patients and in patients failing current antiretroviral therapies. The drug is a small molecule developed for the infectious disease therapeutic area.
MK0518 is developed by Merck & Company, Inc., which trades under the ticker MRK. Merck sponsored the clinical trials evaluating the drug in HIV-infected patients, including studies combining it with other antiretroviral agents such as TRUVADA.
MK0518 has been studied in Phase 3 clinical development. Its trials include a Phase 3 study and two Phase 2 studies, all of which are completed. The drug is investigational and is not described as approved.
MK0518 has been evaluated in completed trials including NCT00369941, a Phase 3 study versus efavirenz in treatment-naive HIV-infected patients; NCT00105157 and NCT00100048, Phase 2 studies in HIV-infected patients; and NCT01000818, a Phase 1 pharmacokinetic study with famotidine and omeprazole.
Yes, MK0518 is also known as raltegravir. Other names used for the same compound include MK-0518 and MK0518 (Raltegravir). Searches for any of these names refer to the same Merck small molecule studied in HIV infection.
MK0518 is a small molecule antiretroviral agent studied for HIV-1 infection and HIV infections. Its trials evaluated antiretroviral activity in treatment-naive patients and in patients failing current antiretroviral therapies, both as monotherapy and in combination regimens.