Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Label indication LYNKUET is indicated for the treatment of moderate to severe vasomotor symptoms (VMS) due to menopause. LYNKUET is a neurokinin 1 (NK1) and neurokinin 3 (NK3) receptor antagonist indicated for the treatment of moderate to severe vasomotor symptoms due to menopause. ( 1 ) FDA label
Also known as Elinzanetant (BAY3427080)
Elinzanetant · 17 trials · 9 indications
Participants' assessments of HF were recorded electronically twice daily using the sponsor developed Hot Flash Daily Diary (HFDD). The HFDD was completed in the morning after waking up (morning diary) and each evening at bedtime (evening diary) on the hand-held device. The HFDD items assessed the number of mild, moderate, and severe HF experienced during the day and during the night. Mild HF was defined as a "sensation of heat without sweating", moderate HF was defined as a "sensation of heat with sweating, but able to continue activity", and severe HF was defined as a "sensation of heat with sweating, causing cessation (stopping) of activity". Mean daily frequency is calculated as total number of moderate to severe HF during that week divided by the total number of available days with data during that week.
Participants' assessments of HF were recorded electronically twice daily using the sponsor developed Hot Flash Daily Diary (HFDD). The HFDD was completed in the morning after waking up (morning diary) and each evening at bedtime (evening diary) on the hand-held device. The HFDD items assessed the number of mild, moderate, and severe HF experienced during the day and during the night. Mild HF was defined as a "sensation of heat without sweating", moderate HF was defined as a "sensation of heat with sweating, but able to continue activity", and severe HF was defined as a "sensation of heat with sweating, causing cessation (stopping) of activity". Mean daily frequency is calculated as total number of moderate to severe HF during that week divided by the total number of available days with data during that week.
Participants' assessments of HF were recorded electronically twice daily using the sponsor developed Hot Flash Daily Diary (HFDD). The HFDD was completed in the morning after waking up (morning diary) and each evening at bedtime (evening diary) on the hand-held device. The HFDD items assessed the number of mild, moderate, and severe HF experienced during the day and during the night. Mild HF was defined as a "sensation of heat without sweating", moderate HF was defined as a "sensation of heat with sweating, but able to continue activity", and severe HF was defined as a "sensation of heat with sweating, causing cessation (stopping) of activity". The frequency of moderate to severe HF for each week during the treatment period was calculated using the available data during that particular week. Specifically, for Week 4, Day 22-28 were used (Day 1 corresponds to start of treatment).
The frequency of moderate to severe HF for each week during the treatment period was calculated using the available data during that particular week. Specifically, for Week 12, Day 78-84 were used (Day 1 corresponds to start of treatment).
In the HFDD, hot flash (HF) severity is scored as 1=mild, 2=moderate, and 3=severe; a decrease indicates improvement. The diary records the number of mild, moderate, and severe HFs during day and night. Mild HFs are a "sensation of heat without sweating"; moderate are "heat with sweating but able to continue activity"; severe are "heat with sweating that stops activity." Baseline mean daily severity is calculated as: (2×moderateHFs+3×severeHFs)÷(totalmoderate+severeHFs).(2 × moderate HFs + 3 × severe HFs) ÷ (total moderate + severe HFs).(2×moderateHFs+3×severeHFs)÷(totalmoderate+severeHFs). If none occur, severity=0. Weekly severity during treatment is based on available days (Week 4: Days 22-28; Week 12: Days 78-84; Day 1=start of treatment), averaging the mean daily severity for that week. If more than 2 days are missing, the weekly value is set to missing
In the HFDD, hot flash (HF) severity is categorized as 1=mild, 2=moderate, 3=severe; thus, a decrease indicates improvement. The HFDD records the number of mild, moderate, and severe HFs during day and night. Mild HFs are a "sensation of heat without sweating"; moderate involve "heat with sweating but able to continue activity"; severe involve "heat with sweating that stops activity." Mean daily severity at baseline is calculated as: (2 × moderate HFs) + (3 × severe HFs)\\\] ÷ (total moderate + severe HFs). If none occur, severity is set to 0. Weekly severity during treatment is based on available days (Week 4: Days 22-28; Week 12: Days 78-84; Day 1=start of treatment), averaging mean daily severity across that week. If more than 2 days are missing, the week is set to missing.
The frequency of moderate to severe HF for each week during the treatment period was calculated using the available data during that particular week. Specifically for Week 4, Days 22-28 were used (Day 1 corresponds to start of treatment). Mean daily frequency is calculated as total number of moderate to severe HF during that week divided by the total number of available days with data during that week
The frequency of moderate to severe HF for each week during the treatment period was calculated using the available data during that particular week. Specifically for Week 12, Days 78-84 were used (Day 1 corresponds to start of treatment). Mean daily frequency is calculated as total number of moderate to severe HF during that week divided by the total number of available days with data during that week
In the HFDD, hot flash (HF) severity is scored as 1=mild, 2=moderate, and 3=severe; a decrease indicates improvement. The diary records the number of mild, moderate, and severe HFs during day and night. Mild HFs are a "sensation of heat without sweating"; moderate are "heat with sweating but able to continue activity"; severe are "heat with sweating that stops activity." Baseline mean daily severity is calculated as: (2×moderateHFs+3×severeHFs)÷(totalmoderate+severeHFs).(2 × moderate HFs + 3 × severe HFs) ÷ (total moderate + severe HFs).(2×moderateHFs+3×severeHFs)÷(totalmoderate+severeHFs). If none occur, severity=0. Weekly severity during treatment is based on available days (Week 4: Days 22-28; Week 12: Days 78-84; Day 1=start of treatment), averaging the mean daily severity for that week. If more than 2 days are missing, the weekly value is set to missing.
In the HFDD, hot flash (HF) severity is categorized as 1=mild, 2=moderate, 3=severe; thus, a decrease indicates improvement. The HFDD records the number of mild, moderate, and severe HFs during day and night. Mild HFs are a "sensation of heat without sweating"; moderate involve "heat with sweating but able to continue activity"; severe involve "heat with sweating that stops activity." Mean daily severity at baseline is calculated as: (2 × moderate HFs) + (3 × severe HFs)\\\] ÷ (total moderate + severe HFs). If none occur, severity is set to 0. Weekly severity during treatment is based on available days (Week 4: Days 22-28; Week 12: Days 78-84; Day 1=start of treatment), averaging mean daily severity across that week. If more than 2 days are missing, the week is set to missing.
The HFDD items assess the number of mild, moderate, and severe HF experienced during the day and during the night. Mild HF are defined as a "sensation of heat without sweating", moderate HF are defined as a "sensation of heat with sweating, but able to continue activity", and severe HF are defined as a "sensation of heat with sweating, causing cessation (stopping) of activity".
WASO is defined as total time (min) spent awake from onset of persistent sleep to lights on. Persistent sleep is defined as 20 consecutive epochs (10 min) of non wakefulness. Smaller WASO values indicate shorter periods of wakefulness after sleep onset.
Participants recorded daily in their electronic diary (eDiary) the frequency and severity of hot flushes during the treatment period. The baseline assessment for hot flushes was calculated using the last 7 days (not necessarily consecutive days) with an available data in the evening and/or the morning of the baseline diary completion period. A diary day was comprised of the evening entry of this day and the morning entry of the following day, in that order. Mean daily frequency = Sum of number of hot flushes filled in the diary during the last 7 diary days (with at least one available data in the evening and/or morning) divided by 7. Moderate: Sensation of heat with sweating, but able to continue activity. Severe: Sensation of heat with sweating, causing cessation (stopping) of activity.
Participants recorded daily in their electronic diary (eDiary) the frequency and severity of hot flushes during the treatment period. The baseline assessment for hot flushes was calculated using the last 7 days (not necessarily consecutive days) with an available data in the evening and/or the morning of the baseline diary completion period. A diary day was comprised of the evening entry of this day and the morning entry of the following day, in that order. Mean daily frequency = Sum of number of hot flushes filled in the diary during the last 7 diary days (with at least one available data in the evening and/or morning) divided by 7. Moderate: Sensation of heat with sweating, but able to continue activity. Severe: Sensation of heat with sweating, causing cessation (stopping) of activity.
Participants recorded daily in their eDiary the frequency and severity of hot flushes during the treatment period. Mean weekly severity = (number of moderate hot flushes for 7 days) x 2 + (number of severe hot flushes for 7 days) x 3\] / (total number of moderate to severe hot flushes over 7 days). Severity is graded by the women from 1 to 3 (1 = mild; 2 = moderate; 3 = severe).
Participants recorded daily in their eDiary the frequency and severity of hot flushes during the treatment period. Mean weekly severity = (number of moderate hot flushes for 7 days) x 2 + (number of severe hot flushes for 7 days) x 3\] / (total number of moderate to severe hot flushes over 7 days). Severity was graded by the women from 1 to 3 (1 = mild; 2 = moderate; 3 = severe).
elinzanetant administered in the evening 3 hours after a light dinner.
elinzanetant administered in the evening 3 hours after a light dinner.
elinzanetant administered in the evening 3 hours after a light dinner.
SDLP: standard deviation of lateral position. CRCDS-MiniSim: Cognitive Research Corporation's Driving Simulator-MiniSim.
Cmax: maximum observed drug concentration in plasma after single dose
AUC(0-tlast) will be the primary endpoint if AUC cannot be determined in all participants. AUC: area under the concentration vs. time curve from zero to infinity after single dose; AUC(0-tlast): area under the concentration vs. time curve from zero to last quantifiable concentration after single dose
AUC(0-tlast) will be used as the main parameter if AUC cannot be reliably determined
AUC from time 0 to the last data point greater than lower limit of quantification (LLOQ) (AUC\[0-tlast\]) will be used as a primary parameter, if AUC cannot be determined in all participants.
Measured matrix after a single dose administration.
Maximum observed (unbound) drug concentration (Cmax,u) in measured matrix after a single dose administration.
(AUC(0-tlast) will be used as main parameter if AUC cannot be calculated.)
(AUC(0-tlast) will be used as main parameter if AUC cannot be calculated.)
AUC: Area under the concentration vs. time curve from zero to infinity after single (first) dose.
AUC: Area under the concentration vs. time curve from zero to infinity after single (first) dose.
Cmax: Maximum observed drug concentration in measured matrix after single dose administration.
Cmax: Maximum observed drug concentration in measured matrix after single dose administration.
AUC: Area under the concentration vs. time curve from zero to infinity after single (first) dose
Cmax: Maximum observed drug concentration in measured matrix after single dose administration
| Arm | Type | Description |
|---|---|---|
| Elinzanetant (BAY3427080) | EXPERIMENTAL | Participants will receive 120 mg elinzanetant orally once daily. |
| Placebo | PLACEBO_COMPARATOR | Participants will receive matching placebo orally once daily for 12 weeks, followed by 120 mg elinzanetant orally once daily |
| Placebo + elinzanetant | PLACEBO_COMPARATOR | Participants will receive matching placebo orally once daily for 12 weeks, followed by elinzanetant 120 mg for 14 weeks. |
| Elinzanetant arm | EXPERIMENTAL | Participants will take Elinzanetant |
| Placebo arm | PLACEBO_COMPARATOR | Participants will take elinzanetant matching placebo |
| 160 mg Elinzanetant (BAY3427080) | EXPERIMENTAL | Participants received 4x40 mg elinzanetant capsules. |
| 120 mg Elinzanetant (BAY3427080) | EXPERIMENTAL | Participants received 3x40 mg elinzanetant capsules and 1 placebo capsule. |
| 80 mg Elinzanetant (BAY3427080) | EXPERIMENTAL | Participants received 2x40 mg elinzanetant capsules and 2 placebo capsules. |
| 40 mg Elinzanetant (BAY3427080) | EXPERIMENTAL | Participants received one 40 mg elinzanetant capsule and 3 placebo capsules. |
| Sequence 1: Treatment A followed by Treatment B | EXPERIMENTAL | Participants receive Treatment A followed by Treatment B in a randomized 2 x 2 crossover design with two treatment periods. |
| Sequence 2: Treatment B followed by Treatment A | EXPERIMENTAL | Participants receive Treatment B followed by Treatment A in a randomized 2 x 2 crossover design with two treatment periods. |
| Treatment sequences A-C-D-B | EXPERIMENTAL | Treatment A (elinzanetant dose A). Treatment B (elinzanetant dose B). Treatment C (zopiclone 7.5 mg). Treatment D (placebo). |
| Treatment sequences B-D-C-A | EXPERIMENTAL | Treatment A (elinzanetant dose A). Treatment B (elinzanetant dose B). Treatment C (zopiclone 7.5 mg). Treatment D (placebo). |
| Treatment sequences C-B-A-D | EXPERIMENTAL | Treatment A (elinzanetant dose A). Treatment B (elinzanetant dose B). Treatment C (zopiclone 7.5 mg). Treatment D (placebo). |
| Treatment sequences D-A-B-C | EXPERIMENTAL | Treatment A (elinzanetant dose A). Treatment B (elinzanetant dose B). Treatment C (zopiclone 7.5 mg). Treatment D (placebo).). |
| EZN - DBG | EXPERIMENTAL | Participants will receive a single oral dose of dabigatran (DBG) etexilate in fasted state in Period 1; followed by a single oral dose of elinzanetant (EZN) and DBG etexilate (30 min after EZN) in fasted state in Period 2. |
| Treatment A-B | EXPERIMENTAL | Participants will receive a single dose of elinzanetant supplied in strength level 1 and 9 subsequent multiple doses from Days 4 to 12 of Period 1; followed by a single dose of elinzanetant supplied in strength level 2 and 9 subsequent multiple doses from Days 4 to 12 of Period 2. |
| Treatment B-A | EXPERIMENTAL | Participants will receive a single dose of elinzanetant supplied in strength level 2 and 9 subsequent multiple doses from Days 4 to 12 of Period 1; followed by a single dose of elinzanetant supplied in strength level 1 and 9 subsequent multiple doses from Days 4 to 12 of Period 2. |
| Moderate renal impairment | EXPERIMENTAL | Participants with estimated glomerular filtration rate (eGFR) of 30 to 59 mL/min/1.73 m\^2 |
| Severe renal impairment | EXPERIMENTAL | Participants with eGFR \< 30 mL/min/ 1.73 m\^2 |
| Normal renal function | EXPERIMENTAL | Participants with ≥ 90 mL/min/1.73 m\^2 |
| Period 1 | EXPERIMENTAL | A single dose of elinzanetant and an additional IV (microtracer dose) of \[13C5\]BAY 3427080 will be administered. |
| Period 2 | EXPERIMENTAL | Once daily oral dose of esomeprazole and a single oral dose of elinzanetant will be administered. |
| Elinzanetant single dose step 1 | EXPERIMENTAL | Each participant will receive a single oral dose of elinzanetant or placebo. |
| Elinzanetant single dose step 2 | EXPERIMENTAL | Each participant will receive a single oral dose of elinzanetant or placebo. |
| Elinzanetant single dose step 3 | EXPERIMENTAL | Each participant will receive a single oral dose of elinzanetant or placebo. |
| Elinzanetant single dose step 4 | EXPERIMENTAL | Each participant will receive a single oral dose of elinzanetant or placebo. |
| Elinzanetant single dose step 6 | EXPERIMENTAL | Each participant will receive a single oral dose of elinzanetant or placebo. |
| Elinzanetant multiple dose step 5 | EXPERIMENTAL | Each participant will receive multiple doses of elinzanetant or placebo administered once a day for 7 consecutive days. |
| Rosuvastatin and/or elinzanetant | EXPERIMENTAL | The participants will receive each dose of rosuvastatin and/or elinzanetant together with 240 mL of non-sparkling water in total. |
| Participants receive study medication on time point 1 | EXPERIMENTAL | Participants will receive two single doses of elinzanetant in two different treatments in a randomized sequence (Treatment A, Treatment B). |
| Participants receive study medication on time point 2 | EXPERIMENTAL | Participants will receive two single doses of elinzanetant in two different treatments in a randomized sequence (Treatment A, Treatment B). |
| Name | Type | Description |
|---|---|---|
| Elinzanetant (BAY3427080) | DRUG | 120 mg elinzanetant orally once daily |
| Placebo | DRUG | Matching placebo orally once daily |
| Elinzanetant | DRUG | Oral |
| Elinzanetant (BAY 3427080) treatment A | DRUG | Elinzanetant treatment A is administered orally once daily. |
| Elinzanetant (BAY 3427080) treatment B | DRUG | Elinzanetant treatment B is administered orally once daily. |
| Placebo to elinzanetant | DRUG | Oral administration |
| Zopiclone | DRUG | Oral administration |
| Placebo to zopiclone | DRUG | Oral administration |
| Dabigatran etexilate | DRUG | Capsule, oral, single dose |
| Esomeprazole | DRUG | Esomeprazole given orally once daily for 5 days in Period 2. |
| Midazolam | DRUG | Midazolam given orally as single dose in Period 1 and in Period 2. |
| Carbamazepine | DRUG | Carbamazepine given orally twice daily in Period 2 . |
| Rosuvastatin | DRUG | Single doses on Day 1, Day 8, and Day 13 |
| Elinzanetant (BAY3427080) treatment A | DRUG | Single oral dose |
| Elinzanetant (BAY3427080) treatment B | DRUG | Single oral dose |
Inclusion Criteria: * Females aged 18 to 70 years of age inclusive, at the time of signing the informed consent. * Women experiencing vasomotor symptoms (VMS) caused by adjuvant endocrine therapy that they are expected to use for the duration of the study * Tamoxifen with or without the use of g...
Elinzanetant is an investigational small-molecule drug developed by Bayer AG for vasomotor symptoms, commonly known as hot flashes, and related conditions. It is being studied in women experiencing menopause, sleep disturbances associated with menopause, and hot flashes caused by anti-cancer therapy in women with or at high risk for hormone-receptor positive breast cancer.
Elinzanetant targets TACR1 and TACR3, which are the neurokinin 1 and neurokinin 3 receptors. It acts as an antagonist at both receptors. By blocking these targets, elinzanetant is designed to modulate the neurokinin pathway implicated in vasomotor symptoms.
Elinzanetant is being developed by Bayer AG, which trades on the OTC market under the ticker BAYRY. Bayer is the sponsor of the clinical trials evaluating the drug.
Elinzanetant is in Phase 2 development according to the overall program status, though individual trials have reached Phase 3. It is investigational and has not been approved by the FDA. Clinical studies include Phase 1, Phase 2, and Phase 3 trials.
Elinzanetant has been studied in multiple clinical trials, including NCT07762287, a Phase 1 trial in healthy female participants; NCT06219902, a Phase 1 trial in healthy women; NCT06112756, a completed Phase 2 trial in women with sleep disturbances associated with menopause; and NCT05587296, a Phase 3 trial in women with hot flashes caused by anti-cancer therapy.
Yes, Elinzanetant is also known as BAY3427080. Other alternative names include Elinzanetant (BAY3427080) treatment A, Elinzanetant treatment A, Elinzanetant (BAY3427080) treatment B, Elinzanetant treatment B, Elinzanetant (BAY 3427080) treatment A, and Elinzanetant (BAY 3427080) treatment B.